Ansari MJ, Ahmed MM, Fatima F, Anwer MK, Jamil S, Al-shdefat R, Ali BE, Al-Awmi F and Abdel-Kader MS. Influence of hydrophilic polymers on complexation and solublizing efficiencies of beta cyclodextrin over silymarin. International Journal of Biology, Pharmacy and Allied Sciences. 2014; 3(10): 237-242. (ISI indexed).
Silymarin exhibits very low bioavailability (23 – 47%) due to its poor aqueous solubility and hence it needs improvement in the solubility and dissolution rate so as to enhance bioavailability and to derive its maximum therapeutic efficacy. Though cyclodextrin complexation and use of water-soluble polymers for enhancing the solubility of silymarin have been investigated separately, no reports are available on their combined use in enhancing the solubility. The objective of the present investigation is to study the complexation of silymarin with β-cyclodextrin alone and in the presence of hydrophilic polymers by phase solubility study and to evaluate the feasibility of enhancing the solubility of silymarin. The aqueous solubility of silymarin was linearly increased as a function of the concentration of β-cyclodextrin alone and in the presence of hydrophilic polymers, PVP, HPMC and PEG 6000. The increase in solubility was due to the formation of a 1: 1 M complexes in solutions. The complexes formed between β-cyclodextrin and silymarin were quite stable as indicated by apparent stability constants. Addition of hydrophilic polymers has markedly enhanced the complexation efficiency of β-cyclodextrin. Of the investigated polymers,PVP has given the highest enhancement in the complexation efficiency of β-cyclodextrin. The order of hydrophilic polymers in enhancing the complexation efficiency was PVP > HPMC > PEG 6000. Hydrophilic polymers have markedly enhanced the solubilizing efficiency of β-cyclodextrin. PVP has given highest enhancement (12.67 fold) in the solublizing efficiency of β-cyclodextrin. Hence, a combination of β-cyclodextrin and hydrophilic polymers is recommended for enhancing solubility of silymarin
Influence of hydrophilic polymers on complexation and solublizing efficiencies of beta cyclodextrin
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