SOLUBILITY ENHANCEMENT OF ROSUVASTATIN VIA NANOSPONGES: PREPARATION AND IN-VITRO CHARACTERIZATION

Main Article Content

Afifa Tariq
Rimsha Liaqat
Pervaiz Akhtar Shah
Hashmat Ullah
Syed Atif Raza
Sheikh Abdur Rashid
Qaiser Iqbal
Aamna Naz
Sadia Haider
Saima Mahmood
Mobina Manzoor
Ghulam Mustafa Khan

Keywords

Rosuvastatin, solubility enhancement, oral bioavailability, nanosponges, in-vitro drug release

Abstract

Rosuvastatin is regarded as super statin and being a member of BCS class Ⅱ exhibit low aqueous solubility and dissolution rate with poor oral bioavailability of less than 20%. The current study involved rosuvastatin loaded nano-sponges preparation utilizing polyvinyl alcohol (surfactant), ethyl cellulose (polymer) while dichloromethane was used as cross linker. Nanosponge represents a scaffold structure of size less than 100 um demonstrating an excellent approach to deliver drugs that are poorly absorbed or show low solubility in GIT. The formulations were crafted by emulsion solvent evaporation method, initially screened via pre-formulation studies and finally were characterized by various physico-chemical tests. FTIR analysis showed no interaction among pure drug and formulation excipients. Zeta experiment revealed the stable formulations having droplet sizes in the range of 270-343 nm further confirmed by SEM indicating the porous sponge like appearance. There were high percent yield values of 80-87% with 62-74% entrapment efficiency of prepared formulations. Additionally dissolution and kinetic model analysis was established on the formulated nano-sponges to further examine their sustained release property, highlighting initial burst release of surface adhered drug followed by controlled release with anomalous non-Fickian diffusion mechanism. The findings of this study advocated successful fabrications of rosuvastatin loaded nanosponges that could improve low solubility and oral bioavailability of the drug.

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References

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