Nanostructured lipid carrier: a potential system for enhanced oral bioavailability of felodipine
By: Patil, Archana Sidagouda
.
Contributor(s): Jaknoor, Vinayak.
Publisher: Karnataka Association of Pharmaceutical Teachers of India (APTI) 2022Edition: Vol.56(1), Jan-Mar.Description: 77-85p.Subject(s): PHARMACEUTICSOnline resources: Click here
In:
Indian journal of pharmaceutical education and researchSummary: 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.
| Item type | Current location | Call number | Status | Date due | Barcode | Item holds |
|---|---|---|---|---|---|---|
Articles Abstract Database
|
School of Pharmacy Archieval Section | Not for loan | 2022-1701 |
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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