In vitro characterization studies of self microemulsified Bosentan systems.

In vitro characterization studies of self microemulsified Bosentan systems.

Drug Dev Ind Pharm. 2017 Jan 25;:1-22

Authors: Vadlamudi HC, Yalavarthi PR, Basaveswara Rao MV, Rasheed A, N T

Abstract
CONTEXT: Bosentan is a poorly soluble drug and pose challenges in design delivery systems.
OBJECTIVE: To enhance the solubility, dissolution and shelf-life of bosentan by formulating it as S-SMEDDS capsules.
MATERIALS AND METHODS: Solubility of bosentan was tested in various liquid vehicles such as oils (rice bran and sunflower), surfactants (span 20 and tween 80) and co-surfactants (PEG 400 and propylene glycol) and microemulsions were developed. Bosentan was incorporated into appropriate microemulsion systems which were previously identified from pseudo ternary phase diagrams. Bosentan loaded SMEDDS were evaluated for drug content, drug release, zeta potential and droplet size. The selected liquid SMEDDS were converted into solid SMEDDS by employing adsorption and melt granulation. Solid SMEDDS were characterized for micromeritics and evaluated for drug content, drug release and shelf-life.
RESULTS: Isotropic systems R5, R13, S5 and S13 with submicron droplet size had exhibited 85.45, 94.12, 81.67 and 96.64% drug release respectively. Solid SMEDDS of MR13 and AS13 formulations with rapid reconstitution ability, they exhibited 84.85 and 86.74% of on par drug release. The formulations were physicochemically intact for 1.02 and 1.56 years.
DISCUSSION: Liquid SMEDDS composed with PEG400 had displayed optimal characters. Solid SMEDDS had high dissolution profiles than bosentan due to modification in the crystalline structure of drug upon microemulsification.
CONCLUSION: Thus, solid SMEDDS addressed the solubility, dissolution and stability issues of bosentan and becomes an alternate for clinical convenience.

PMID: 28121194 [PubMed - as supplied by publisher]

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