Design, Optimization, and Characterization of Atorvastatin-Loaded Lipid-based Carriers for Enhanced Oral Bioavailability

Indian Journal of Pharmaceutical Education and Research

  • Mohini Mondal1Department of Pharmaceutical Technology, JIS University, Agarpara, Kolkata, West Bengal, INDIA.
  • Biplab Debnath2Department of Pharmaceutical Technology, Bharat Technology, Uluberia, Howrah, West Bengal, INDIA.
  • Swarupananda Mukherjee3Department of Pharmaceutics, NSHM Knowledge Campus, Kolkata - Group of Institutions, 124, B.L Saha Road, Kolkata, West Bengal, INDIA.
  • Tapan Kumar Shaw1Department of Pharmaceutical Technology, JIS University, Agarpara, Kolkata, West Bengal, INDIA.

Volume 60 Issue 4s Pages s1772-s1781

DOI: 10.5530/ijper.20264022

Abstract

Aim: This study presents a dose reduction with sustained action and increased bioavailability. Atorvastatin (ATV) is the drug of choice for the management of hyperlipidemia, and the commonly available marketed product of ATV is tablets. ATV is a poorly water-soluble drug showing with a low oral bioavailability (approximately 12%). The first-pass metabolism of ATV is another cause of its low bioavailability. Nanoliposome of ATV increases bioavailability, hypothesizing the reduction of metabolism by reducing free exposure of the drug and protecting it from metabolizing enzymes) and increase their solubility due to the greater surface area of tiny nanoliposome of ATV. Nanoiposomes are tiny spherical vesicles with one or more lipid bilayers composed of physiological lipids. Materials and Methods: In this study, Nanoliposome of ATV were prepared by the thin film hydration Method: In analytical grade Atorvastatin (ATV), Cholesterol (CHL), Soybean Phosphatidylcholine (SPC), Tween, Acetonitrile purchased from Merck and characterized by vesicle size, size distribution, and drug loading efficiency. The preliminary investigation of batches was designed using a 32 full factorial design, with the size and drug loading as dependent variables. Results: The formulation batch 3 (NL3) showed liposomes 110.3 ± 14.6 nm in size with PDI value 0.28 ±0.03 and zeta potential -58.7 ± 7.1 with drug loading more than 60% and this batch was considered the optimized one. Further, this batch will be studied for its shape by FESEM and lamellarity by cryo-TEM analysis, and the justification of the increase in bioavailability was carried out in the selected animal model by HPLC. Thus, it is possible to administer drugs via experimentally generated nano liposomes, which could be an effective method to enhance bioavailability. Conclusion: New Study presents few folds higher drug bioavailability using nano carriers. In conclusion, the fabricated Nano liposomes of ATV may be a useful strategy for enhancing the bioavailability of ATV.

Keywords

  • Atorvastatin
  • Nano-liposome
  • Bioavailability Enhancement
  • Liposomal Formulation
  • In vitro-Study
  • Statistical Analysis
  • In vivo-Study
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