Relevant bibliographies by topics / Lipophilic drug

Academic literature on the topic 'Lipophilic drug'

Author: Grafiati
Published: 10 December 2022
Last updated: 28 January 2023

Create a spot-on reference in APA, MLA, Chicago, Harvard, and other styles

Select a source type:

Contents

Consult the lists of relevant articles, books, theses, conference reports, and other scholarly sources on the topic 'Lipophilic drug.'

Next to every source in the list of references, there is an 'Add to bibliography' button. Press on it, and we will generate automatically the bibliographic reference to the chosen work in the citation style you need: APA, MLA, Harvard, Chicago, Vancouver, etc.

You can also download the full text of the academic publication as pdf and read online its abstract whenever available in the metadata.

Journal articles on the topic "Lipophilic drug"

1

Gulati, Monica, Manish Grover, Saranjit Singh, and Mandip Singh. "Lipophilic drug derivatives in liposomes." International Journal of Pharmaceutics 165, no. 2 (May 1998): 129–68. http://dx.doi.org/10.1016/s0378-5173(98)00006-4.

Full text
APA, Harvard, Vancouver, ISO, and other styles
2

Esteves-Pedro, Natalia Mencacci, Kenji Sugibayashi, Elissa A. Ostrosky, Marcio Ferrari, Bianca da Silva Sufi, Monica Beatriz Mathor, Paulo Roberto H. Moreno, et al. "Validation Cytotoxicity Assay for Lipophilic Substances." Current Topics in Medicinal Chemistry 18, no. 4 (May 29, 2018): 275–86. http://dx.doi.org/10.2174/1568026618666180410142829.

Full text
Abstract:
It is challenging to disperse lipophilic substances in a validated cytotoxicity assay, especially for compounds with log Kow greater than or equal to 5 that may show false negative results. The purpose of this study was to explain the challenges in conducting a cytotoxicity validated test of lipophilic substances: Minthostachys setosa, Pimenta pseudocaryophyllus, and Drimysbrasiliensis essential oils. Additionally, we compared the equivalence of Neutral Red (NR) and 3- (4,5-dimethylthiazol-2-yl) -5- (3- carboxymethoxyphenyl) -2- (4-sulfophenyl) -2H -tetrazolium, inner salt (MTS) in detecting cell viability. The Hydrophile-Lipophile Balance (HLB) technique was used to evaluate the dispersion of essential oils and cytotoxicity in accordance to the guidelines of the OECD / GD 129 validated cytotoxicity assay. We compared the equivalence of vital dyes by TOST equivalence test. According to the results, we demonstrated the possibility of using other ways to disperse the lipophilic substances. Based on the HLB theory, we selected polysorbate 20 as the best solubilizing agent of the essential oils studied in D10 culture medium.
APA, Harvard, Vancouver, ISO, and other styles
3

Peixoto, F. S., P. M. Dias, G. A. Ramaldes, J. M. C. Vilela, M. S. Andrade, and A. S. Cunha. "Atomic Force Microscopy Applied to the Characterization of Solid Lipid Nanoparticles." Microscopy and Microanalysis 11, S03 (December 2005): 52–55. http://dx.doi.org/10.1017/s1431927605050877.

Full text
Abstract:
Solid lipid nanoparticles (SLN) have generated increasing attention as an alternative carrier system, particularly for lipophilic drugs [1-2]. The system consists of lipid nanoparticles, which are solid at room temperature. The solid matrix offers the possibility to improve the stability against coalescence and the reduced mobility of incorporated drug molecules is a pre requisite for controlled drug release [3]. Dexamethasone acetate was used as a model drug because of its wide application in the pharmaceutical field and lipophilic properties.
APA, Harvard, Vancouver, ISO, and other styles
4

Kayipmaz, Afsin Emre, Betul Gulalp, and Sibel Benli. "Current Aspects in Lipophilic Drug Toxicity." Journal of Academic Emergency Medicine 10, no. 2 (June 1, 2011): 80–85. http://dx.doi.org/10.5152/jaem.2011.019.

Full text
APA, Harvard, Vancouver, ISO, and other styles
5

Arun Kumar, Kapil Kumar, Aparna Joshi, Ikram, and Deepak Teotia. "A Comprehensive review on Niosome: a prominent carrier in advance drug delivery." GSC Biological and Pharmaceutical Sciences 18, no. 1 (January 30, 2022): 093–99. http://dx.doi.org/10.30574/gscbps.2022.18.1.0033.

Full text
Abstract:
Niosomes are vesicular nacarriers that can be used for both amphiphilic and lipophilic drugs. Niosomes are budding vehicles in advanced drug delivery systems. Niosomes are nionic surfactants vesicles that can be formed with or without the addition of cholesterol. Niosomes can be the best choice for nacarriers because of their specific characters like biodegradability, biocompatibility, and immugenic nature. Niosomes can easily trap the hydrophilic and lipophilic drugs and extend the period of the drug in the systemic circulation. Niosomes are the nacarrier that can enhance penetration of drugs into the specific target tissues hence resulting in reduced toxicity. The main aim of this review article is to provide a detailed description of Niosomes.
APA, Harvard, Vancouver, ISO, and other styles
6

Zielińska, Aleksandra, Amanda Cano, Tatiana Andreani, Carlos Martins-Gomes, Amélia M. Silva, Marlena Szalata, Ryszard Słomski, and Eliana B. Souto. "Lipid-Drug Conjugates and Nanoparticles for the Cutaneous Delivery of Cannabidiol." International Journal of Molecular Sciences 23, no. 11 (May 31, 2022): 6165. http://dx.doi.org/10.3390/ijms23116165.

Full text
Abstract:
Lipid nanoparticles are currently used to deliver drugs to specific sites in the body, known as targeted therapy. Conjugates of lipids and drugs to produce drug-enriched phospholipid micelles have been proposed to increase the lipophilic character of drugs to overcome biological barriers. However, their applicability at the topical level is still minimal. Phospholipid micelles are amphiphilic colloidal systems of nanometric dimensions, composed of a lipophilic nucleus and a hydrophilic outer surface. They are currently used successfully as pharmaceutical vehicles for poorly water-soluble drugs. These micelles have high in vitro and in vivo stability and high biocompatibility. This review discusses the use of lipid-drug conjugates as biocompatible carriers for cutaneous application. This work provides a metadata analysis of publications concerning the conjugation of cannabidiol with lipids as a suitable approach and as a new delivery system for this drug.
APA, Harvard, Vancouver, ISO, and other styles
7

Nalawade, Vishwajit, and Kunal Patil. "Liposome: A Novel Drug Delivery System." International Journal of Research Publication and Reviews 04, no. 01 (2022): 1795–801. http://dx.doi.org/10.55248/gengpi.2023.4148.

Full text
Abstract:
Liposome was derived from two Greek words “Lipos meaning fat and Soma meaning body”. Liposome were spherical shaped vesicles consist of phospholipids and cholesterol. Due to their size hydrophobic and lipophilic character they are very promising system for drug delivery. This novel drug delivery system aims to target the drug directly to the site of action. Liposomes are very biocompatible and stable and have unique property to entrap both hydrophilic drug and lipophilic drug to its compartment and lead to controlled release effect. They are of 0.05- 5.0 micrometer in diameter. Liposomes are used for the treatment of various diseases like tumors or cancer. Liposomal Drug Delivery System and various aspects related to liposome that can be studied Compared with traditional drug delivery systems, liposomes exhibit better properties, including site-targeting, sustained or controlled release, protection of drugs from degradation and clearance, superior therapeutic effects, and lower toxic side effects. This review describes liposomes structure, composition, preparation methods, and evaluation clinical applications
APA, Harvard, Vancouver, ISO, and other styles
8

Suresh Babu P, Marina Amarendra, Subha V J, and Senthamarai S. "An analytical assessment on Mucoadhesive Buccal Drug Delivery System for improving patient convenience and compliance." International Journal of Research in Pharmaceutical Sciences 11, SPL4 (December 20, 2020): 252–58. http://dx.doi.org/10.26452/ijrps.v11ispl4.3780.

Full text
Abstract:
In recent years, the novel mucoadhesive buccal drug delivery system has been developed over the conventional and systemic dosage forms. To bypass drugs from the hepatic first-pass metabolism and it enhances the bioavailability of drug at the site of administration. Absorption of a drug through the buccal mucosa reduces the degradation. Some of the enzyme activity and pH variation in the gastrointestinal tract reduces the absorption and active drug loss. To overcome this problem, the buccal route is preferred. Polymers are used in this formulation to improve the drug release rate over an extended period, and also, the therapeutic plasma level of the drug can be rapidly achieved. Overall this narrative review explains mechanism and theories, method of preparation, factors affecting mucoadhesion, advantages and limitations, applications, components used in the formulation, characterization and evaluation methods. Since the cytoplasm and intercellular spaces are hydrophilic. Lipophilic drugs have a low solubility in this environment. However, the cell membrane is rather lipophilic; it tends to difficulty permeating the hydrophilic solute through the cell membrane because of a low partition coefficient. Therefore, the cytoplasm and intercellular spaces act as a major barrier to penetration of lipophilic compounds and the cell membrane poses as an extensive transport barrier for hydrophilic compounds. Since the oral epithelial is stratified, the permeation of solute may involve these combination routes so that the route is more predictable.
APA, Harvard, Vancouver, ISO, and other styles
9

Charman, William N. "Lipids, Lipophilic Drugs, and Oral Drug Delivery—Some Emerging Concepts." Journal of Pharmaceutical Sciences 89, no. 8 (August 2000): 967–78. http://dx.doi.org/10.1002/1520-6017(200008)89:8<967::aid-jps1>3.0.co;2-r.

Full text
APA, Harvard, Vancouver, ISO, and other styles
10

Hegde, Rahul Rama, Anurag Verma, and Amitava Ghosh. "Microemulsion: New Insights into the Ocular Drug Delivery." ISRN Pharmaceutics 2013 (June 27, 2013): 1–11. http://dx.doi.org/10.1155/2013/826798.

Full text
Abstract:
Delivery of drugs into eyes using conventional drug delivery systems, such as solutions, is a considerable challenge to the treatment of ocular diseases. Drug loss from the ocular surface by lachrymal fluid secretion, lachrymal fluid-eye barriers, and blood-ocular barriers are main obstacles. A number of ophthalmic drug delivery carriers have been made to improve the bioavailability and to prolong the residence time of drugs applied topically onto the eye. The potential use of microemulsions as an ocular drug delivery carrier offers several favorable pharmaceutical and biopharmaceutical properties such as their excellent thermodynamic stability, phase transition to liquid-crystal state, very low surface tension, and small droplet size, which may result in improved ocular drug retention, extended duration of action, high ocular absorption, and permeation of loaded drugs. Further, both lipophilic and hydrophilic characteristics are present in microemulsions, so that the loaded drugs can diffuse passively as well get significantly partitioned in the variable lipophilic-hydrophilic corneal barrier. This review will provide an insight into previous studies on microemulsions for ocular delivery of drugs using various nonionic surfactants, cosurfactants, and associated irritation potential on the ocular surface. The reported in vivo experiments have shown a delayed effect of drug incorporated in microemulsion and an increase in the corneal permeation of the drug.
APA, Harvard, Vancouver, ISO, and other styles
More sources

Dissertations / Theses on the topic "Lipophilic drug"

1

Quader, Sabina, and N/A. "Selective Synthetic Modification of Aminoglycosides for Drug Targeting to Tuberculosis." Griffith University. School of Biomolecular and Physical Sciences, 2007. http://www4.gu.edu.au:8080/adt-root/public/adt-QGU20071024.151619.

Full text
Abstract:
The work presented in this thesis details the synthetic modification of the clinically important aminoglycoside antibiotics, neomycin B, paromomycin and tobramycin. We sought to modify aminoglycosides by attaching lipophilic groups, including fatty acids and steroids, with a view to improving the bacterial membrane permeability of these species, and ultimately their efficacy in the treatment of tuberculosis. Our initial synthetic strategy involved direct and specific functionalization of the singular primary hydroxyl group of the aminoglycoside antibiotic neomycin B, with lipophilic groups containing carboxylic acid functions via Mitsunobu esterification. Although, direct and selective Mitsunobu acylation of the primary hydroxyl group proved unsuccessful in the case of the pseudo tetrasaccharide neomycin B, the Mitsunobu reaction did however result in selective chemistry elsewhere in the molecule and this has been exploited for modification of the ido (ring IV) and streptamine (ring II) ring systems. Under carefully controlled conditions, the Mitsunobu reaction has been used for the selective dehydration of the ido ring, to give the talo epoxide, and, under more forcing Mitsunobu dehydration conditions, an aziridine function has been introduced into the streptamine moiety. Both the epoxide and the epoxide-aziridine neomycin building blocks were utilized as synthons in subsequent chemical transformations. Seventeen novel neomycin derivatives featuring modification of ring IV and/or ring II were obtained using this approach. Explicit structural elucidation of all the synthetic intermediates and the final products was achieved using high temperature NMR spectroscopy. Direct and specific functionalization of the singular primary hydroxyl group at the C5 position of the ribose ring (ring III) of neomycin B was achieved, via a procedure based in part on selective tripsylation of the C5III primary hydroxyl group of neomycin B reported previously, followed by subsequent displacement of the tripsyl group by azide. Terminal alkyne containing lipophilic esters were then successfully attached to the ribose residue of neomycin B via Cu(I)-mediated azide-alkyne coupling reaction. In addition to the isolation of two fortuitous, new and versatile synthons i.e. monoanhydro neomycin and bis-anhydro neomycin for modification of ring IV and ring II of neomycin, a third synthon based on neomycin framework, allowing stepwise modification of ring III and ring IV was designed and synthesized. This synthon features an epoxide function in the ido ring, and a protected amine function at the C5 position of the ribose ring. Examples of the stepwise use of this synthon for further synthetic modification of the neomycin framework were demonstrated. Fourteen novel neomycin derivatives featuring modification of ring III and /or ring IV were obtained and characterized. Regioselective Mitsunobu esterification of the single primary hydroxyl group of the pseudo trisaccharide tobramycin was utilized successfully to link a variety of hydrophobic esters with tobramycin. Nine lipophilic tobramycin derivatives with significant structural diversity were synthesised and characterized. In a preliminary study, the applicability of the Mitsunobu dehydration reaction for the regioselective formation of an epoxide ring in the ido moiety of the pseudo tetrasaccharide aminoglycoside antibiotic paromomycin system was confirmed. The regioselective ring-opening of the derived epoxide with azide at C3IV of paromomycin was also successfully demonstrated. In total, forty-two new potential aminoglycoside antibiotics have been synthesized and characterized.
APA, Harvard, Vancouver, ISO, and other styles
2

Nyakas, Claudia Verfasser], Karsten [Akademischer Betreuer] [Mäder, Reinhard H. H. [Akademischer Betreuer] Neubert, and Wolfgang J. [Akademischer Betreuer] Parak. "Polyelectrolyte nanocapsules as modern drug delivery system for lipophilic drug candidates / Claudia Nyakas. Betreuer: Karsten Mäder ; Reinhard Neubert ; Wolfgang J. Parak." Halle, Saale : Universitäts- und Landesbibliothek Sachsen-Anhalt, 2012. http://d-nb.info/1025352858/34.

Full text
APA, Harvard, Vancouver, ISO, and other styles
3

Dawoud, Mohamed [Verfasser], Alfred [Akademischer Betreuer] Fahr, Heike [Akademischer Betreuer] Bunjes, and Thomas [Akademischer Betreuer] Rades. "Investigations on the transfer of lipophilic drug models from lipid nanoparticles to lipophilic acceptor compartments using different techniques / Mohamed Dawound. Gutachter: Alfred Fahr ; Heike Bunjes ; Thomas Rades." Jena : Thüringer Universitäts- und Landesbibliothek Jena, 2011. http://d-nb.info/1016368259/34.

Full text
APA, Harvard, Vancouver, ISO, and other styles
4

Vázquez, Lozano Javier. "On the usage of lipophilic descriptors for molecular similarity evaluation." Doctoral thesis, Universitat de Barcelona, 2019. http://hdl.handle.net/10803/667608.

Full text
Abstract:
Three-dimensional ligand-based virtual screening methods have been used for many years in drug discovery, with a variable success depending on different factors, such as the complexity of the target system or the suitability of the molecular descriptors. New approaches are still necessary to cover the broad spectrum of relationships that a drug-like molecule may establish with the organism. In spite of the complexity of processes that modulate the activity of a drug, most tools are primarily focused on the use of shape or electrostatic descriptors. In contrast, since the importance of lipophilicity in pharmacodynamics and pharmacokinetics process, an exact representation of the 3D pattern of hydrophobic/hydrophilic regions can be a valuable guideline to enhance the molecular similarity studies. In this scenario, PharmScreen was conceived as a tool to exploit lipophilic 3D similarity. Exploiting the MST contributions to octanol/water partition coefficients, the capacity to perform correct molecular overlays and distinguish between active and inactive molecules is discussed. The overlap algorithm is validated against the AstraZeneca test, which comprises 121 experimentally derived sets of molecular overlays. The results point out the suitability of the MST-based hydrophobic parameters for generating molecular overlays, as correct predictions were obtained for 94%, 79%, and 54% of the molecules classified into easy, moderate, and hard sets, respectively. Moreover, the results point out that this accuracy is attained at a much lower degree of identity between the templates used by hydrophobic/HB fields and electrostatic/steric ones. On the other hand, the topological hydrophobic descriptors proposed are applied over 3D-QSAR models. In this context, the Miertus–Scrocco–Tomasi-derived hydrophobic descriptors have been shown to provide models for structure–activity relationships with a predictive accuracy comparable to traditional techniques based on electrostatic/steric parameters. The results reported support the assumption that lipophilicity, supplemented by HB acceptors/donors, provides a useful signature to enrich the information that can be retrieved from (i) molecular alignment and (ii) QSAR models, complementing the results obtained traditionally from electrostatic and steric properties. Taken together, lipophilicity is presented as a valuable alternative for the molecular similarity study. In addition, the applicability of our descriptors in structure-based methods has been explored in order to re-evaluate the complexes constituted by docking techniques (in our case, Glide). Since (de)solvation is fundamental for the establishment of the ligand-receptor complex, it can be expected that the docked ligands in the same pocket share lipophilic characteristics, even if there are several binding modes. However, approximations that affect solvation contribution are applied in the docking score functions, and by extension, some docking programs show problems performing VS especially in hydrophobic binding pockets. Specific binding typically requires the formation of key interactions between targets and ligands. Thus, 3D similarity relative to experimental binding modes could be sufficient to distinguish active compounds from decoys. In view of the results obtained the similarity descriptors proposed are introduced as a valid scoring function for discerning between active and inactive compounds. These findings support the usefulness of lipophilicity as driver descriptors in molecular similarity studies promoting their use in virtual screening campaigns considering LB approaches or in combination with SB. As conclusion, results obtained from the analysis of hydrophobic/hydrophilic descriptors presented in this thesis opens a new window to explore the vast chemical space, complementing the information derived from traditional descriptors in ligand- and structure-based approaches.
El fet d'assumir que molècules estructuralment semblants donaran lloc a activitats biològiques similars ha estat una idea àmpliament explotada en el disseny de fàrmacs. Aquesta premissa subjau en la majoria de les aplicacions pràctiques en recerca química i farmacèutica. No obstant això, el concepte de similitud molecular és subjectiu i la seva interpretació pot variar segons l’ús que se’n vulgui derivar. La quantificació d’aquesta mesura de semblança molecular depèn de la representació de les característiques químiques presents en l'estructura molecular mitjançant descriptors 1D, 2D o 3D, la ponderació d'aquests descriptors i l'expressió matemàtica de la funció de similitud. En l’àmbit de les característiques químiques utilitzades en els mètodes tridimensionals de similitud molecular, les propietats electrostàtiques i estèriques han estat dominants tradicionalment. Tanmateix, això oculta el paper fonamental exercit per altres contribucions a l'afinitat d'unió, com els canvis en la (de)solvatació del lligant i del receptor. Malgrat la seva rellevància, la lipofilicitat ocupa aparentment un paper secundari com a descriptor principal del reconeixement lligand-receptor. Sota aquesta premissa s’ha desenvolupat una eina de cribratge virtual 3D basada en lligands (PharmScreen) que explota les relacions de similitud entre topologies hidrofòbiques derivades del model continuo de solvatació Miertus – Scrocco – Tomasi (MST). Els estudis reportats al llarg d’aquesta tesis recolzen la utilitat de les contribucions atòmiques a la lipofilicitat com a descriptors fonamentals en estudis de similitud, complementant la informació derivada dels descriptors tradicional. PharmScreen es presenta, així, com una eina competitiva per aplicar en campanyes de cribratge virtual basada en lligand o en combinació amb tècniques basades en proteïna, obrint una nova finestra en l’ampli espai químic.
APA, Harvard, Vancouver, ISO, and other styles
5

Schuck, Virna Josiane Aurelio. "Use of microdialysis as a tool to determine tissue distribution of lipophilic and high molecular weight compounds." [Gainesville, Fla.] : University of Florida, 2004. http://purl.fcla.edu/fcla/etd/UFE0008003.

Full text
Abstract:
Thesis (Ph.D.)--University of Florida, 2004.
Typescript. Title from title page of source document. Document formatted into pages; contains 139 pages. Includes Vita. Includes bibliographical references.
APA, Harvard, Vancouver, ISO, and other styles
6

Eley, John Graham. "The incorporation of lipophilic agents into low density lipoprotein for drug targeting and evaluation as anticancer delivery systems." Thesis, University of Strathclyde, 1989. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.278421.

Full text
APA, Harvard, Vancouver, ISO, and other styles
7

Croughton, Karen. "Novel pharmacology of the lipophilic antifolate methylbenzoprim." Thesis, University of Nottingham, 2001. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.368236.

Full text
APA, Harvard, Vancouver, ISO, and other styles
8

Cheung, Wai-Han. "Novel steroidal metal complexes with potential pharmaceutical applications." Thesis, Loughborough University, 1992. https://dspace.lboro.ac.uk/2134/27879.

Full text
Abstract:
A study to develop novel lipophilic metal ion complexes based on dihydrocholesterol was undertaken. Steroid ligands functionalised at the 2- and 3- positions were synthesized as possible bidentate ligands for complexation of metal ions. Condensation of 5α-cholestan-3-one with ethyl formate in the presence of base gave 2-hydroxymethylene-5α-cholestan-3-one, and 2- acetyl-5α-cholestan-3-one was obtained by the reaction between 3- trimethylsilyloxy-5α-cholest-2-ene and acetyl chloride. Attempts to synthesize 2,3-dioximino-5α-cholestane from 5α-cholestan-3-one and 2α-hydroxy-5α-cholestan-3-one were unsuccessful. Likewise 2- methylene-5α-cholestan-3-one, which was expected to lead to other bidentate ligands, could not be prepared satisfactorily from 5α-cholestan- 3-one or 3-trimethylsilyloxy-5α-cholest-2-ene.
APA, Harvard, Vancouver, ISO, and other styles
9

Drooge, Dirk Jan van. "Combining the incompatible inulin glass dispersions for fast dissolution, stabilization and formulation of lipophilic drugs /." [S.l. : [Groningen : s.n.] ; University Library Groningen] [Host], 2006. http://irs.ub.rug.nl/ppn/29297678X.

Full text
APA, Harvard, Vancouver, ISO, and other styles
10

Kattner, Sven-Desiderius [Verfasser], Dagmar [Gutachter] Fischer, Gerhard [Gutachter] Scriba, and Oliver [Gutachter] Germershaus. "Entwicklung von PLGA-Nanopartikeln als Drug Delivery System für lipophile Wirkstoffe, die in die Arachidonsäurekaskade eingreifen / Sven-Desiderius Kattner ; Gutachter: Dagmar Fischer, Gerhard Scriba, Oliver Germershaus." Jena : Friedrich-Schiller-Universität Jena, 2020. http://d-nb.info/1223981711/34.

Full text
APA, Harvard, Vancouver, ISO, and other styles
More sources

Books on the topic "Lipophilic drug"

1

(Editor), Vladimir Pliska, Bernard Testa (Editor), Han Van De Waterbeemd (Editor), and Han Van De Waterbeemd (Editor), eds. Lipophilicity in Drug Action and Toxicology. John Wiley & Sons, 1996.

Find full text
APA, Harvard, Vancouver, ISO, and other styles
2

Columb, Malachy O. Local anaesthetic agents. Edited by Michel M. R. F. Struys. Oxford University Press, 2017. http://dx.doi.org/10.1093/med/9780199642045.003.0017.

Full text
Abstract:
Local anaesthetic agents cause a pharmacologically induced reversible neuropathy characterized by axonal conduction blockade. They act by blocking the sodium ionophore and exhibit membrane stabilizing activity by inhibiting initiation and propagation of action potentials. They are weak bases consisting of three components: a lipophilic aromatic ring, a link, and a hydrophilic amine. The chemical link classifies them as esters or amides. Local anaesthetics diffuse through the axolemma as unionized free-base and block the ionophore in the quaternary ammonium ionized form. The speed of onset of block is therefore dependent on the pKa of the agent and the ambient tissue pH. Esters undergo hydrolysis by plasma esterases and amides are metabolized by hepatic microsomal mixed-function oxidases. Local anaesthetics are bound in the blood to α‎1-acid glycoproteins. Pharmacological potency is dependent on the lipid solubility of the drug as is the potential for systemic toxicity. The blood concentrations required to cause cardiovascular system (CVS) collapse and early central nervous system (CNS) toxicity are used to quantify the CVS:CNS toxicity ratio. Local anaesthetics also have the potential to induce direct neuronal damage. Intravenous lipid emulsion is used for the treatment of systemic toxicity but the scientific evidence is inconsistent. With regard to the pipecoloxylidine local anaesthetics, early evidence indicated that the S- was less toxic than the R-enantiomer. However, clinical research using minimum local analgesic concentration designs suggests that reduced systemic toxicity and motor block sparing is mainly explained by potency rather than enantiomerism.
APA, Harvard, Vancouver, ISO, and other styles
3

Lipophilicity in drug action and toxicology /edited by Vladimir Pliška, Bernard Testa, and Han van de Waterbeemd. Weinheim: VCH, 1996.

Find full text
APA, Harvard, Vancouver, ISO, and other styles
4

Servin, Frédérique S., and Valérie Billard. Anaesthesia for the obese patient. Edited by Philip M. Hopkins. Oxford University Press, 2017. http://dx.doi.org/10.1093/med/9780199642045.003.0087.

Full text
Abstract:
Obesity is becoming an epidemic health problem, and the number of surgical patients with a body mass index of more than 50 kg m−2 requiring anaesthesia is increasing. Obesity is associated with physiopathological changes such as metabolic syndrome, cardiovascular disorders, or sleep apnoea syndrome, most of which improve with weight loss. Regarding pharmacokinetics, volumes of distribution are increased for both lipophilic and hydrophilic drugs. Consequently, doses should be adjusted to total body weight (propofol for maintenance, succinylcholine, vancomycin), or lean body mass (remifentanil, non-depolarizing neuromuscular blocking agent). For all drugs, titration based on monitoring of effects is recommended. To minimize recovery delays, drugs with a rapid offset of action such as remifentanil and desflurane are preferable. Poor tolerance to apnoea with early hypoxaemia and atelectasis warrant rapid sequence induction and protective ventilation. Careful positioning will prevent pressure injuries and minimize rhabdomyolysis which are frequent. Because of an increased risk of pulmonary embolism, multimodal prevention is mandatory. Regional anaesthesia, albeit technically difficult, is beneficial in obese patients to treat postoperative pain and improve rehabilitation. Maximizing the safety of anaesthesia for morbidly obese patients requires a good knowledge of the physiopathology of obesity and great attention to detail in planning and executing anaesthetic management. Even in elective surgery, many cases can be technical challenges and only a step-by-step approach to the avoidance of potential adverse events will result in the optimal outcome.
APA, Harvard, Vancouver, ISO, and other styles

Book chapters on the topic "Lipophilic drug"

1

Gozes, Illana, and Mati Fridkin. "Lipophilic vasoactive intestinal peptide: Potential drug for non-invasive impotence treatment." In Peptide Chemistry 1992, 442–45. Dordrecht: Springer Netherlands, 1993. http://dx.doi.org/10.1007/978-94-011-1474-5_131.

Full text
APA, Harvard, Vancouver, ISO, and other styles
2

Carrara, M., S. D’Ancona, and L. Cima. "An Inert Mixture for Solubilizing Lipophilic Drugs in Cell Culture Assays." In Mechanisms and Models in Toxicology, 338–43. Berlin, Heidelberg: Springer Berlin Heidelberg, 1987. http://dx.doi.org/10.1007/978-3-642-72558-6_67.

Full text
APA, Harvard, Vancouver, ISO, and other styles
3

Mansbach, Charles M., and Anne Arnold. "Physiological Responses of Intestinal CTP: Phosphocholine Cytidylyltransferase and its Interaction with Lipophilic Drugs." In Enzymes of Lipid Metabolism II, 65–69. Boston, MA: Springer US, 1986. http://dx.doi.org/10.1007/978-1-4684-5212-9_9.

Full text
APA, Harvard, Vancouver, ISO, and other styles
4

Gao, Ping. "Design and Development of Self-Emulsifying Lipid Formulations for Improving Oral Bioavailability of Poorly Water-Soluble and Lipophilic Drugs." In Formulating Poorly Water Soluble Drugs, 243–66. New York, NY: Springer New York, 2011. http://dx.doi.org/10.1007/978-1-4614-1144-4_7.

Full text
APA, Harvard, Vancouver, ISO, and other styles
5

Natarajan, Jawahar, and Veera Venkata Satyanarayana Reddy Karri. "Formulation and Comparison of Lipophilic Drugs Through Self-Emulsifying Pellets Using Extrusion–Spheronization Technique." In Nanoparticles in Polymer Systems for Biomedical Applications, 176–202. Oakville, Canada ; Waretown, NJ : Apple Academic Press, [2019]: Apple Academic Press, 2018. http://dx.doi.org/10.1201/9781351047883-7.

Full text
APA, Harvard, Vancouver, ISO, and other styles
6

Amitai, Gabriel, Eliezer Rachaman, Rachel Adani, Ishai Rabinovitz, Rachel Brandeis, and Eliahu Heldman. "Quaternary-Lipophilic Carbamates with Blood Brain Barrier Permeability as Potential Drugs for Memory Impairment Associated with Cholinergic Deficiency." In Advances in Behavioral Biology, 595–600. Boston, MA: Springer US, 1998. http://dx.doi.org/10.1007/978-1-4615-5337-3_84.

Full text
APA, Harvard, Vancouver, ISO, and other styles
7

Amitai, G., R. Adani, I. Rabinovitz, G. Sod-Moriah, R. Brandeis, E. Rachaman, and E. Heldman. "Quaternary-Lipophilic Carbamates with Blood Brain Barrier Permeability as Potential Drugs for the Treatment of Diseases Associated with Cholinergic Deficiency." In Structure and Function of Cholinesterases and Related Proteins, 277–82. Boston, MA: Springer US, 1998. http://dx.doi.org/10.1007/978-1-4899-1540-5_81.

Full text
APA, Harvard, Vancouver, ISO, and other styles
8

Sultana, Nazneen, Juber Akhtar, Badruddeen, Mohammad Irfan Khan, Usama Ahmad, Muhammad Arif, Mohammad Ahmad, and Tanmay Upadhyay. "Nanoemulgel: For Promising Topical and Systemic Delivery." In Drug Development Life Cycle [Working Title]. IntechOpen, 2022. http://dx.doi.org/10.5772/intechopen.103878.

Full text
Abstract:
Nanoemulgel delivery system is a fusion of two different delivery systems, wherein the physical state of drug containing nanoemulsion is changed by adding it to the gel matrix, thus enabling more lipophilic drugs to be used in treatment therapies. It solves the major issues such as limiting use of lipophilic drugs, poor oral bioavailability, and unpredictable pharmacokinetic and absorption variations. Simultaneously, its nongreasy nature and easily spreading ability support the patient compliance. Nanoemulgel can be widely used in the treatment of acne, pimple, psoriasis, fungal infection, and inflammation cause by osteoarthritis and rheumatoid arthritis. The delivery of drug via ocular, vaginal, dental, and nose to brain routes for the treatment of diverse local and systemic ailments for instance alopecia, periodontitis, and Parkinson’s are possible. In the cosmetic industries, UV absorber nanoemulgel protected skin from sunburn.
APA, Harvard, Vancouver, ISO, and other styles
9

Hoffman, Amnon, and Arik Dahan. "Enhanced Gastrointestinal Absorption of Lipophilic Drugs." In Enhancement in Drug Delivery. CRC Press, 2006. http://dx.doi.org/10.1201/9780849332036.ch6.

Full text
APA, Harvard, Vancouver, ISO, and other styles
10

"Enhanced Gastrointestinal Absorption of Lipophilic Drugs." In Enhancement in Drug Delivery, 126–47. CRC Press, 2006. http://dx.doi.org/10.1201/9781420004816-12.

Full text
APA, Harvard, Vancouver, ISO, and other styles

Conference papers on the topic "Lipophilic drug"

1

Kooiman, Klazina, Marcel R. Bohmer, Marcia Emmer, Hendrik J. Vos, Ceciel Chlon, William T. Shi, Christopher S. Hall, et al. "Oil-filled polymeric ultrasound contrast agent as local drug delivery system for lipophilic drugs." In 2008 IEEE Ultrasonics Symposium (IUS). IEEE, 2008. http://dx.doi.org/10.1109/ultsym.2008.0082.

Full text
APA, Harvard, Vancouver, ISO, and other styles
2

Sureau, F., J. M. Kuhnel, M. A. Schwaller, and Pierre-Yves Turpin. "Cellular mechanisms of lipophilic cationic drug distribution: a confocal laser microspectrofluorometric assessment." In Laser Applications in Life Sciences: 5th International Conference, edited by Pavel A. Apanasevich, Nikolai I. Koroteev, Sergei G. Kruglik, and Victor N. Zadkov. SPIE, 1995. http://dx.doi.org/10.1117/12.197407.

Full text
APA, Harvard, Vancouver, ISO, and other styles
3

Sukhenko, Liudmila, Elsayed Zeitar, Anna Fedotova, and Mikhail Egorov. "Prospects of naked licorice cultivation in the caspian region for the creation of foam licorice baths (based on the drug glytsrfit)." In Innovations in Medical Science and Education. Dela Press Publishing House, 2022. http://dx.doi.org/10.56199/dpcsms.bjse2063.

Full text
Abstract:
The prospects of cultivation of naked licorice in the territory of the Caspian region and the possibility of using extractive saponin-containing foaming components of licorice root to create foam licorice baths with foam content stability were studied. The latitude, longitude, and height of licorice root collection sites with row furrows are presented only in rows. A new approach to preserving the hydrophilic-lipophilic balance in a licorice bath is proposed by embedding colloidal surfactants into the micelles of licorice root saponins, which increases the stability of licorice foam in the bath. The data of the critical concentration of micelle formation are presented. The possibility of restoring the stocks of licorice naked during its cultivation and harvesting by the row method is shown, and methods for preserving the solubilizing ability of foam licorice baths under conditions of preserving licorice foam micelles in the presence of some surfactants are disclosed.
APA, Harvard, Vancouver, ISO, and other styles
4

Wang, C. T., J. Y. Lee, J. C. Chen, Y. J. Shiao, and W. J. Tsai. "EFFECT OF TRIFLUOPERAZINE (TFP) ON HUMAN PLATELET MEMBRANE." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1644816.

Full text
Abstract:
TFP is a lipophilic antipsychotic drug. The drug will first encounter with cell membrane when adding it into a cell suspension. The effect of TFP on plasma membrane of the gel-filtered human platelet was investigated by : 1) scanning electron microscopy (SEM); 2) measuring theleakiness of marker enzymes and compound; 3) estimating its solubility in membrane. The cells were suspended in the modified Tyrode's buffer containing 0.1% dextrose, 0.2% of bovine serum albumin and without calcium. The SEM study showed that platelet changed shape from disc to ellipsoid in 10 μM TFP.,Increasingthe TFP concentration from 20 μM to 50 μM resulted in changing thecell from ellipsoid to sphere with a wavy surface. The drug did not cause any significant change in the cell volume. TFPof 70 μM caused platelet becoming a round ball shape with a spongy-like cell surface. 100 μM TFP caused more than 90% of cells to lyse and to agglutinate with each other. The time courseof morphological change of the TFP-affected platelets showed that the cellsswelled into irregular shape within 2 min. Apparent leakiness of serotonin was observed at 20 μM TFP, while the leakages of both lactate dehydrogenase and acid hydrolase were found at 40 μM TFP. The TFP uptake study showed that platelet was permeable to TFP by simple diffusion. The partition coefficient of TFP in platelet membrane was estimated to be 1 x 104. These results indicate that TFP molecules are solubilized in membrane. The extent in perturbation of the membrane structure depends on concentration of the drug used. (This research was supported by a grant from the National Science Council of the Republic of China.)
APA, Harvard, Vancouver, ISO, and other styles
5

Tartis, Michaelann S., Jan Marik, Azadeh Kheirolomoom, Rachel E. Pollard, Hua Zhang, Jinyi Qi, Julie L. Sutcliffe, and Katherine W. Ferrara. "Pharmacokinetics of Encapsulated Paclitaxel: Multi-Probe Analysis With PET." In ASME 2007 Summer Bioengineering Conference. American Society of Mechanical Engineers, 2007. http://dx.doi.org/10.1115/sbc2007-176435.

Full text
Abstract:
We have combined two imaging probes and used PET as a means to provide image-based validation for a novel targeted drug delivery system. The first probe was a direct labeling of the drug [18F]fluoropaclitaxel [1–3], which was inserted into various carrier vehicle formulations. The second probe, [18F]fluoro-1,2-dipalmitoyl-sn-glycerol, i.e. [18F]FDP involved radiolabeling the lipid vehicle. Paclitaxel, which is poorly soluble in aqueous media, also has limited solubility and stability in lipophilic environments such as liposomes. Stable association of paclitaxel with the lipid bilayer is affected by a variety of physicochemical factors such as temperature and liposome composition. Paclitaxel crystal formation has been documented, with two forms of solid state within aqueous media and organic solvents, although crystal conformation differs in each media [4,5]. We provide dynamic in vivo image sets providing biodistribution and time activity curves of free [18F]fluoropaclitaxel and liposomal [18F]fluoropaclitaxel as well as free [18F]FDP, liposomal [18F]FDP, and [18F]FDP in an ultrasound contrast agent. Serial studies were performed within a small group of rats, minimizing inter-animal variability. The two labeled molecules have different biodistributions: paclitaxel is rapidly taken up in the liver, intestines and kidneys, while the labeled lipid incorporated into liposomes stays in circulation with minimal uptake in organs other than spleen. Here, we have developed a quantitative method to follow paclitaxel and lipid vehicles to their destination in vivo in order to improve targeted paclitaxel delivery.
APA, Harvard, Vancouver, ISO, and other styles
6

Kovalev, Igor S., Leila K. Sadieva, Olga S. Taniya, Victoria M. Yurk, Artem S. Minin, Dmitry S. Kopchuk, Grigory V. Zyryanov, et al. "Pyrene-based lipophilic/biphilic chemosensors for the fluorescence “turn-off” detection of nitroanalytes in aqueous media." In MODERN SYNTHETIC METHODOLOGIES FOR CREATING DRUGS AND FUNCTIONAL MATERIALS (MOSM2020): PROCEEDINGS OF THE IV INTERNATIONAL CONFERENCE. AIP Publishing, 2021. http://dx.doi.org/10.1063/5.0068657.

Full text
APA, Harvard, Vancouver, ISO, and other styles
7

Couffin, Anne-Claude, Thomas Delmas, Jean-Sébastien Thomann, Ismail Cheibani, Eric Bayma, Emilie Heinrich, Marie Escudé, et al. "Physical and chemical gels of lipid nanoparticles for controlled delivery of lipophilic drugs and proteins." In SPIE Microtechnologies, edited by Angeliki Tserepi, Manuel Delgado-Restituto, and Eleni Makarona. SPIE, 2013. http://dx.doi.org/10.1117/12.2016880.

Full text
APA, Harvard, Vancouver, ISO, and other styles
You might also be interested in the extended bibliographies on the topic 'Lipophilic drug' for particular source types:
Journal articles Dissertations / Theses
We offer discounts on all premium plans for authors whose works are included in thematic literature selections. Contact us to get a unique promo code!

To the bibliography