Silymarin-laden PVP-PEG polymeric composite for enhanced aqueous solubility and dissolution rate: Preparation and in vitro characterization

Publication date: Available online 19 September 2018Source: Journal of Pharmaceutical AnalysisAuthor(s): Abid Mehmood Yousaf, Usman Rashid Malik, Yasser Shahzad, Tariq Mahmood, Talib HussainAbstractThe intent of this work was to develop, optimize and characterize a silymarin-laden polyvinylpyrrolidone (PVP)-polyethylene glycol (PEG) polymeric composite to resolve low aqueous solubility and dissolution rate problem of the drug. A number of silymarin-laden polymeric formulations were fabricated with different quantities of PVP K-30 and PEG 6000 via the solvent-evaporation method. The effect of PVP K-30 and PEG 6000 on the aqueous solubility and dissolution rate was investigated. The optimized formulation and its constituents were characterized using PXRD, DSC, SEM and FTIR techniques. Both the PEG 6000 and PVP K-30 positively affected the aqueous solubility and dissolution rate of the drug. In particular, a formulation consisting of silymarin, PVP K-30 and PEG 6000 (0.25/1.5/1.5, m/m/m) furnished the highest solubility (24.39 ± 2.95 mg/mL) and an excellent dissolution profile (~100% in 40 min). The solubility enhancement with this formulation was ~1150-fold as compared to plain silymarin powder. Moreover, all the constituents existed in the amorphous state in this silymarin-laden PVP-PEG polymeric composite. Accordingly, this formulation might be a promising tool to administer silymarin with enhanced effect via the oral route.Graphical abstract
Source: Journal of Pharmaceutical Analysis - Category: Drugs & Pharmacology Source Type: research