Enhancement of Bioavailability Performance using Solid-self Microemulsifying Drug Delivery System for High Molecular Weight Drug| Chapter 1 | Challenges and Advances in Pharmaceutical Research Vol. 6

 Bosentan Hydrochloride (BOS) has a large molecular weight, only a little water solubility, and eleven hydrogen bond acceptors. It has a low bioavailability as a result. BOS has recently undergone successful development of a new Solid-Self Emulsifying Drug Delivery System (S-SMEDDS) to increase its oral bioavailability by enhancing its solubility and permitting high molecular weight of BOS absorption. Capmul MCM as the oil, Tween 20 as the surfactant, and Propylene glycol as a co-surfactant were found to be suitable for the development of Liquid-Self Emulsifying Drug Delivery System based on solubility, pseudoternary phase diagram, emulsifying efficiency, and compatibility tests (L-SMEDDS). The formulation of the BOS loaded L-SMEDDS was created using various oil, surfactant, and co-surfactant concentrations, and it was then optimised using a variety of evolutionary parameters, including drug content, robustness to dilution, ultrasonic interferometer, ease of emulsification, droplet size, and in vitro diffusion studies. By using a spray drying process, the improved L-SMEDDS were transformed into freely flowing granules. The characterisation of S-SMEDDS powder revealed no interactions between the medication and excipients. Variable concentrations of immediately compressible excipients were used to compress the S-SMEDDS powder. Both the pre-compression and post-compression parameters used S-SMEDDS formulas. An in vitro drug release research showed that all S-SMEDDS tablets significantly enhanced the drug's rate of dissolution when compared to the commercial formulation. The Cmax and AUC of BOS significantly increased when compared to the market formulation during in vivo experiments in Sprague-Dowley rats for the improved formulation (P>0.05). Thus, the current study increased BOS's oral bioavailability.

Author(s) Details:

Sandeep C. Atram,
Vidyabharati College of Pharmacy, Amravati, Maharashtra-444602, India.

Vikrant P. Wankhade,
Vidyabharati College of Pharmacy, Amravati, Maharashtra-444602, India.

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