Lipid based approach for bioavailability enhancement of boswellia serrata

Rakesh Mishra, Shubham Paldewar, Tanaji Nandgude

Dr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pune, Maharashtra, India

ABSTRACT

In past numerous studies reported the potential effect of Boswellia serrata in the treatment of various topical and systemic inflammatory diseases. Despite of potential pharmacological effects the oral delivery of BS is challenging due to poor bioavailability limiting its clinical applications. The objective of this study was to formulate and optimize lipid-based sustained release pellets of Boswellia serrata in order to improve solubility and oral bioavailability. Initially, solid dispersions were formulated by fusion method using hydrophilic grade lipids Gelucire 44/14 and 50/13 in different ratio (1: 0.25, 1: 0.5, 1:0.75, 1:1, and 1:2 w/w). Extrusion spheronization technique was used to further formulate solid dispersion of Boswellia serrata into sustained release pellets utilizing hydrophobic grade lipid carrier gelucire 43/01 and ethyl cellulose as a release retarding agent. Using a 3-level, 2-factor factorial design, the effect of the amount of gelucire 43/01 and ethyl cellulose was investigated and optimized. Compared to pure drug, solid dispersion of Boswellia serrata (batch-F9) demonstrated a 5-fold increase in aqueous solubility and dissolution behavior. The optimum system (batch-F16) achieved a maximum drug release of 95.69 % in 6 hours. In comparison to the marketed preparation, pharmacokinetic investigation in male Wistar rats revealed a 2.52-fold improvement in relative bioavailability of the optimized formulation. The obtained BS lipid-based pellets could be a promising choice for its efficient use in various clinical applications. The developed system could be effectively applied to deliver other phytochemicals having potential pharmacological effects but limited clinical use due to poor bioavailability.

Keywords:

Boswellia serrata, Gelucire, Solid dispersion, Pellets, Spheronization, Bioavailability