Development of Atorvastatin Calcium Biloaded Capsules for Oral Administration of Hypercholesterolemia

Evid Based Complement Alternat Med. 2022 May 16:2022:4995508. doi: 10.1155/2022/4995508. eCollection 2022.

Abstract

The goal of this study was to develop atorvastatin (ATN) calcium biloaded, i.e., immediate release (IR) and sustained release (SR) capsules that would promote the quick onset of action and a better dissolution profile on both the IR and SR aspects. The IR granules were prepared by the wet granulation method, and an aqueous solubility study proved that the IR granules released the ATN within 25 min compared to the pure drug due to the addition of PEG and super disintegrants such as croscarmellose (CC) and crospovidone (CP). The sustained release nanoparticles (SR-NPs) were synthesized using a solvent evaporation technique and an optimal combination of hydrophilic and hydrophobic polymers. The addition of a hydrophobic polymer to a hydrophilic polymer delays drug release, resulting in a sustained and controlled release lasting up to 12 hours. The drug release of ATN from SR nanoparticles followed the Higuchi and Korsmeyer-Peppas models and had first-order kinetics (r2 = ???). Fourier transform infrared spectrophotometry, powder X-ray diffraction, and differential scanning calorimetric analysis were used to test the prepared biloaded capsules, and the results showed that there was no significant interaction between the polymers, excipients, and drug. The SEM and DLS analysis clearly demonstrated that drug particles in a continuous layer were enclosed by polymers at the nanoscale. To summarise, integrating both layers into a single capsule resulted in a superior release profile and patient compliance. Finally, prepared biloaded capsules were discovered to exhibit both an IR and an SR profile.

Publication types

  • Retracted Publication