Nanostructured Lipid Carrier: A Potential System for Enhanced Oral Bioavailability of Felodipine

Background: Felodipine is BCS class II drug with poor and variable bioavailability due to its insolubility in water (19mg/L) and extensive metabolism in liver and gut. Thus, in the study Nanostructured lipid carriers (NLCs) of Felodipine were formulated to improve its solubility and bioavailability. 

Methods: NLCs loaded with Felodipine were prepared by high shear homogenization with ultrasonication. The NLCs were characterized for particle size, polydispersity index, entrapment efficiency, content of drug, in vitro drug release studies, stability studies and in vivo bioavailability studies.

Results: The mean particle size and polydispersity index for optimized formulation F2 was found to be 187.0±0.06 and 0.259±0.002 respectively. The drug content achieved was between the ranges of 51.15± 0.01 to 69.14±003% for F1 to F5 formulations. The zeta potential of optimized formulation was found to be -38.2 mV, which showed good stability. Formulation F2 showed highest percentage entrapment efficiency of 75.15±0.003. In vitro drug release studies showed sustained release pattern with maximum drug release of 72.82% by F2 formulation at the end of 12h. The bioavailability studies demonstrated significant enhancement in bioavailability of Felodipine NLCs in comparison to marketed product. Stability studies carried out for optimized formulation F2 showed that the NLCs are more stable at 4±2°C.

Conclusion: Nanostructured lipid carriers loaded with Felodipine were able enhance the bioavailability of drug by 2.0 folds in comparison to marketed product and also demonstrated sustained drug release pattern for longer period of time.

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Materials: Felodipine pure drug was obtained as a free gift sample from Cipla Pvt. Ltd. Bangalore, India. Compritol ATO 888 was obtained by Gattefosse, France. Oleic acid was purchased from S.D Fine Chemicals, Mumbai, India. Poloxamer 188 was purchased from Ozone International, Mumbai, India. Dialysis membrane with molecular weight cut off of 12000-14000 Dalton was purchased from Hi Media Laboratories Pvt. Ltd. Mumbai, India. All the other chemicals used were of analytical grade.

Article information: Archana Sidagouda Patil, Vinayak Jaknoor, Anand Panchakshari Gadad, Rajashree Shashidhar Masareddy, Panchaxari Mallappa Danadagi, Udaykumar Bolmal. Indian Journal of Pharmaceutical Education and Research, 2022; 56(1):77-85. doi:10.5530/ijper.56.1.10, https://www.semanticscholar.org/paper/Nanostructured-Lipid-Carrier%3A-A-Potential-System-of-Patil-Jaknoor/b95b7b090ba13f18a5c6411b9ff736cac04c7b54