溶解度
溶解
泊洛沙姆
生物利用度
化学
色谱法
溶剂
泊洛沙姆407
核化学
有机化学
共聚物
药理学
聚合物
医学
作者
Amruta S. Tambe,Nancy Pandita
标识
DOI:10.1016/j.jddst.2017.11.025
摘要
Boswellic acids (BAs) a group of pentacyclic triterpenes have therapeutic activities. However, their lipophilic nature limits their aqueous solubility and thus bioavailability. Hence, present study aims to enhance solubility and dissolution of BA by solid dispersion (SD) technique using poloxamer (PXM) 188 and 407 as hydrophilic polymeric carriers. Effect of increasing concentration of PXMs on solubility of BAs was examined using phase solubility studies. The stability constants were 1667.5 M-1 (BA: PXM 188) and 3707.4 M-1 (BA: PXM 407) with an AL type curve. Negative Gibbs free energy (ΔGtr°) values indicated spontaneous nature of BA solubilization which decreased with increasing concentration of carrier demonstrating favorability of reaction. 1:1 and 1:2 SDs synthesized using kneading (KN) and solvent evaporation (SE) method were subjected to physicochemical characterization by FTIR and DSC to assess solid state interactions between BAs and PXMs that suggested interaction between carrier and BAs. Efficiency of PXMs was evaluated using saturated solubility and in vitro drug release studies. SDs of PXM 188 (1:2) and PXM 407(1:1) by KN showed highest solubility and drug release profile indicating ability of PXMs as solubility enhancers of BAs. Thus, SD technique helps improve the solubility and dissolution rate of poorly soluble BAs.
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