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The aim of this study was to enhance the solubility of rosuvastatin (RST) calcium by developing β-cyclodextrin-g-poly(2-acrylamido-2-methylpropane sulfonic acid [AMPS]) hydrogel microparticles through aqueous free-radical polymerization technique. Prepared hydrogel microparticles were characterized for percent entrapment efficiency, solubility studies, Fourier transform infrared spectroscopy, differential scanning calorimetry, thermal gravimetric analysis, powder X-ray diffraction, scanning electron microscopy, zeta size and potential, swelling and release studies. Formulations (HS1–HS9) have shown entrapment efficiency between 83.50%±0.30% and 88.50%±0.25%, and optimum release was offered by formulation HS7 at both pH levels, ie, 1.2 (89%) and 7.4 (92%). The majority of microparticles had a particle size of less than 500 µm and zeta potential of −37 mV. Similarly, optimum solubility, ie, 10.66-fold, was determined at pH 6.8 as compared to pure RST calcium, ie, 7.30-fold. In vivo studies on fabricated hydrogel microparticulate system in comparison to pure drug were carried out, and better results regarding pharmacokinetic parameters were seen in the case of hydrogel microparticles. A potential approach for solubility enhancement of RST calcium and other hydrophobic moieties was successfully developed.

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Solubility of poorly water‐soluble drugs is one of the most emerging issue associated with these drugs to form a suitable dosage form that will provide desired pharmacological response. Their low solubility causes elimination of most of the drug from body as such, and desired therapeutic levels are not achieved. Polymers are major players in these formulations, e.g., chitosan, polyvinyl pyrolidone, polyvinyl alcohol, β‐cyclodextrin, etc. β‐Cyclodextrin is one of the most efficient polymer among all of these to work as a carrier for these drugs to enhance solubility. In the present work, microparticles were prepared by different techniques to enhance solubility of rosuvastatin calcium. Microparticles were evaluated for Fourier transform infrared spectroscopy (FTIR), thermal analysis, dissolution studies, powder X‐ray diffraction (PXRD), scanning electron microscopy (SEM), and stability studies to confirm enhancement in solubility. Different in vitro kinetic models such as zero order, first order, Higuchi, and Korsmeyer–Peppas were applied to determine the release behavior of drug from prepared formulations. Results were statistically analyzed by the one‐way ANOVA test, and the p value was determined to check significant results. Results of PXRD had shown that drug nature was changed from crystalline to amorphous, and FTIR and thermal analysis confirmed that the complex was formed between drug and β‐cyclodextrin. SEM images had shown that microparticles had small size loaded with drug. Results had shown that formulation F3 prepared by solid dispersion of drug and β‐cyclodextrin in 1:3 had achieved maximum release of drug 97% within 45 min.