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ABSTRACT
Title |
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‘Screening of Safflower Oil Microemulsion for Enhancing Bioavailability of Lovastatin’ |
Authors |
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Sujit Arun Desai, Rishikesh Ajit Mohite, Ashok A. Hajare |
Keywords |
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Microemulsion, Bioavailability, Lovastatin |
Issue Date |
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January 2015 |
Abstract |
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Objective: Microemulsions have been widely studied to enhance the bioavailability of the poorly soluble drugs. They have very low surface tension and small droplet size which results in high absorption and permeation. Interest in these versatile carriers is increasing and their applications have been diversified to various administration routes in addition to the conventional oral route. This can be attributed to their unique solublization properties and thermodynamic stability which has drawn attention for their use as novel vehicles for drug delivery
Method: Lovastatin is systemic lipid lowering drug belonging to statins and is used for lowering blood cholesterol. Like all statins, lovastatin works by inhibiting 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA reductase). Pseudoternary phase diagram was constructed to determine the ME existing zone. Optimised ME was evaluated for its transparency, droplet size, zeta potential, viscosity, conductivity, percentage assay, and phase separation study. Solubilisation capacity of the ME system was also determined. An accelerated stability study of optimised
ME was carried out to check the stability of the formulation. The prepared ME was compared with the pure drug solution and commercially available lovastatin tablet for in vitro drug release. Comparative oral absorption of lovastatin from the ME and suspension of the commercially available lovastatin was investigated through an in vivo study in a rat model.
Result: Hence microemulsion produced by water titration method showed good particle size (95nm). Refractive index and % transmittance showed good isotropic formulation. In vitro drug release studies revealed overall increase in release from micro-emulsion compared to lovastatin marketed tablet formulation microemulsion showed 76.72% release and marketed formulation showed 52.3% release. There is no physical interaction between drug and excipients, hence collectively it shows microemulsion is promising drug delivery system. |
Page(s) |
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28-49 |
ISSN |
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0975-9492 |
Source |
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Vol. 6, No.1 |
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