The effect of different oils on the absorption of probucol in the rat

Palin, K.J.; Wilson, Clive G.

doi:10.1111/j.2042-7158.1984.tb04919.x

Cited by 99 publications

(36 citation statements)

References 8 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…It was reported that probucol had high lymphatic bioavailability when coadministrated with lipids. 19,20 Chylomicrons (CMs) are important in drug delivery since many lipophilic drugs are carried by CMs and transported in lymph. 21 Palin and Wilson reported that digestion of oil within the small intestine resulted in the liberation of long-chain fatty acids, which effectively promoted chylomicron formation and consequently the lymphatic transport of DDT or probucol.…”

Section: Bioavailability Studymentioning

confidence: 99%

Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation

Fang¹

2012

IJN

View full text Add to dashboard Cite

Abstract:The objective of our investigation was to design a self-microemulsifying drug-delivery system (SMEDDS) to improve the bioavailability of probucol. SMEDDS was composed of probucol, olive oil, Lauroglycol FCC, Cremophor EL, Tween-80, and PEG-400. Droplet sizes were determined. In vitro release was investigated. Pharmacokinetics and bioavailability of probucol suspension, oil solution, and SMEDDS were evaluated and compared in rats. Plasma drug concentration was determined by high-performance liquid chromatography. After administration of probucol suspension, plasma drug concentration was very low. Relative bioavailability of SMEDDS was dramatically enhanced in an average of 2.15-and 10.22-fold that of oil solution and suspension, respectively. It was concluded that bioavailability of probucol was enhanced greatly by SMEDDS. Improved solubility and lymphatic transport may contribute to the enhancement of bioavailability.

show abstract

Section: Bioavailability Studymentioning

confidence: 99%

Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation

Fang¹

2012

IJN

View full text Add to dashboard Cite

show abstract

“…Oleic acid was chosen as the oil phase in all three lipid formulations as it is the principal long-chain fatty acid that occurs in human mixed intestinal lipids (Staggers et al 1990) and in recognition of the potential merits of longchain unsaturated fatty acids, particularly oleic acid, in the design of a lymphotropic lipid delivery systems (Palin & Wilson 1984;Charman & Stella 1986b).…”

Section: Introductionmentioning

confidence: 99%

A comparison of intestinal lymphatic transport and systemic bioavailability of saquinavir from three lipid-based formulations in the anaesthetised rat model

Griffin

O’Driscoll

2006

Journal of Pharmacy and Pharmacology

View full text Add to dashboard Cite

Saquinavir is a lipophilic, poorly water-soluble HIV protease inhibitor that undergoes extensive firstpass metabolism and exhibits poor oral bioavailability. Redirection of the absorption pathway of anti-HIV compounds from the portal blood to the HIV-rich intestinal lymphatics may enhance therapeutic efficacy and reduce the extent of the first-pass effect. This study investigates the potential of targeted intestinal lymphatic transport of saquinavir via a lipid formulation approach. Three formulations containing oleic acid were examined: cremophor-oleic acid mixed micelles, D-alpha tocopheryl polyethylene glycol 1000 succinate (TPGS)-oleic acid mixed micelles and an oleic acid microemulsion. The mesenteric lymph duct cannulated anaesthetised rat model was employed. Plasma and lymph samples were analysed by HPLC. Lymph triglyceride was measured using an enzymatic colorimetric technique. The extent of lymphatic transport from the lipid vehicles was 0.025-0.05% of the dose administered. The microemulsion produced higher and more prolonged mesenteric lymph concentrations than the micellar formulations. A strong correlation existed between the concentration of saquinavir in intestinal lymph and lymph triglyceride levels. The systemic bioavailability was estimated to be 8.5% and 4.8% for the cremophor mixed micelle and the microemulsion, respectively. The cremophor mixed micelles produced higher bioavailability than TPGS mixed micelles, implying that the nature of the surfactant can influence the distribution of drug between lymph and plasma.

show abstract

“…Enhanced drug absorption was reported when using LCT (long chain triglycerides) compared to MCT (medium chain triglycerides) in SMEDDS (22,23); however, this cannot be taken as a rule.…”

Section: Chemism Of Lipidsmentioning

confidence: 97%

Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs

Čerpnjak¹,

Zvonar²,

Gašperlin³

et al. 2013

Acta Pharmaceutica

186

View full text Add to dashboard Cite

Low oral bioavailability as a consequence of low water solubility of drugs is a growing challenge to the development of new pharmaceutical products. One of the most popular approaches of oral bioavailability and solubility enhancement is the utilization of lipid-based drug delivery systems. Their use in product development is growing due to the versatility of pharmaceutical lipid excipients and drug formulations, and their compatibility with liquid, semi-solid, and solid dosage forms. Lipid formulations, such as self-emulsifying (SEDDS), self-microemulsifying SMEDDS) and self--nanoemulsifying drug delivery systems (SNEDDS) were explored in many studies as an efficient approach for improving the bioavailability and dissolution rate of poorly water-soluble drugs. One of the greatest advantages of incorporating poorly soluble drugs into such formulations is their spontaneous emulsification and formation of an emulsion, microemulsion or nanoemulsion in aqueous media. This review article focuses on the following topics. First, it presents a classification overview of lipid-based drug delivery systems and mechanisms involved in improving the solubility and bioavailability of poorly water-soluble drugs. Second, the article reviews components of lipid-based drug delivery systems for oral use with their characteristics. Third, it brings a detailed description of SEDDS, SMEDDS and SNEDDS, which are very often misused in literature, with special emphasis on the comparison between microemulsions and nanoemulsions.Keywords: lipid-based drug delivery systems (LBDDS), self-emulsifying drug delivery systems (SEDDS), self--microemulsifying drug delivery systems (SMEDDS), self-nanoemulsifying drug delivery systems (SNEDDS), microemulsions, nanoemulsions

show abstract

The effect of different oils on the absorption of probucol in the rat

Cited by 99 publications

References 8 publications

Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation

Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation

A comparison of intestinal lymphatic transport and systemic bioavailability of saquinavir from three lipid-based formulations in the anaesthetised rat model

Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs

Contact Info

Product

Resources

About