DEVELOPMENT OF SELF NANO-EMULSIFYING DRUG DELIVERY SYSTEM FOR AN ANTI-HYPERTENSIVE AGENT FELODIPINE: A SYSTEMATIC APPROACH FOR LIPID NANO-FORMULATION WITH IMPROVED ORAL BIOAVAILABILITY IN RATS

Abstract

Objective: The present study involves the development of SNEDDS employing essential oils for enhancing biopharmaceutical performance.


Methods: Preliminary investigations suggested the selection of cinnamon oil as an essential oil, tween 60 as a surfactant, while transcutol HP as a cosolvent for formulating SNEDDS. Formulations evaluated for stability, robustness to dilution, and emulsification time, droplet size, zeta potential (ζ), cloud point, in vitro drug release, drug excipient compatibility, TEM, stability assessment and in vivo pharmacokinetic performance in rats.


Results: All formulations were robust, stable, and revealed excellent emulsification time<40 s, with fine droplet size (11.41±2.41 nm), lower PDI (0.028-0.277). Formulation F(FLD)6 exhibited a release of 97.7% within 4h, and TEM photograph confirmed spherical droplets. The bioavailability results revealed a higher rate and extent of absorption, AUC, and Cmax for the formulations found to be 1212.4 and 355.40±13.67 (p<0.05). The results recommend that the developed formulation approach offers bioavailability enhancement of FLD.


Conclusion: The study concluded that SNEDDS would be an effective formulation system in increasing the aqueous solubility and potentially bioavailability. Furthermore, it can be applied for other therapeutic categories of drugs belonging to BCS class II and IV that show comparable biopharmaceutical challenges.

Keywords: Felodipine, Essential oils, Bioavailability enhancement, Self-nano emulsifying systems, Pharmacokinetic study

Author Biographies

K. TRIDEVA SASTRI, GITAM Institute of Pharmacy, GITAM Deemed to be University, Rushikonda, Visakhapatnam, Andhra Pradesh State, India

Pharmaceutics

GITAM Institute of Pharmacy

G. V. RADHA, GITAM Institute of Pharmacy, GITAM Deemed to be University, Rushikonda, Visakhapatnam, Andhra Pradesh State, India

Associate Professor,

Department of Pharmaceutics,

GITAM Institute of Pharmacy,

GITAM Deemed to be University

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SASTRI, K. T., & RADHA, G. V. (2020). DEVELOPMENT OF SELF NANO-EMULSIFYING DRUG DELIVERY SYSTEM FOR AN ANTI-HYPERTENSIVE AGENT FELODIPINE: A SYSTEMATIC APPROACH FOR LIPID NANO-FORMULATION WITH IMPROVED ORAL BIOAVAILABILITY IN RATS. International Journal of Applied Pharmaceutics, 12(3), 86-94. https://doi.org/10.22159/ijap.2020v12i3.37203
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