The objective of the present investigation was to design and optimize lipid based floating multiparticulate of Berberine hydrochloride (BERH), so as to increase its solubility and to reduce P-Glycoprotein mediated efflux in the intestine hence to improve oral bioavailability. Solid dispersions were prepared using hydrophilic carriers gelucire 44/14 and gelucire 50/13 in different ratio. The prepared solid dispersion of BERH was further formulated into sustain release gastroretentive floating pellets using hydrophobic lipid carrier gelucire 43/01 as release retardant, sodium bicarbonate (NaHCO3) and hydroxylpropyl methyl cellulose K4M (HPMC K4M) as gas former and matrix polymer respectively. The effect of amount of gelucire 43/01 and NaHCO3 : HPMC K4M were studied and optimized using , a 3-level, 2-factor, factorial design. Solid dispersion of BERH compared to pure drug showed 4 fold enhancement in aqueous solubility. The optimum system could float for more than 8h and showed 88.46% drug release in 8 h. The pharmacokinetic study conducted in male Wistar rats indicated 2.32 fold increase in relative bioavailability of optimized formulation compare to marketed tablet. The lipid based floating pellets of BERH was obtained and could be an applicable choice to deliver BERH with improved bioavailability in effective use for various clinical applications.
Key words: Berberine Hydrochloride; gelucire; solid dispersion; lipid floating multiparticulate; gastroretentive
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