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.
Highlights
Felodipine (FLD) is a Biopharmaceutical Classification System (BCS) class II, belonging to a therapeutic category of anti-hypertensive [1]
Our current study aims to formulate FLD loaded Self-nano-emulsifying drug delivery system (SNEDDS) for enhancement of its solubility, dissolution
Among various essential oils employed, the highest solubility was observed in cinnamon oil (i.e. 281±1.07 mg/ml)
Summary
Felodipine (FLD) is a Biopharmaceutical Classification System (BCS) class II, belonging to a therapeutic category of anti-hypertensive [1]. Due to its susceptibility towards hepatic metabolism and lipophilicity, FLD has poor oral bioavailability. The oral route is preferred by its potential physiological aids, besides patient compliance. Various formulation systems were developed for enhancing FLD oral bioavailability, including microparticles, solid dispersions, and nanoparticles [2, 3]. Oral lipid-based formulation systems have gained much significance in enhancing the solubility, followed by oral bioavailability of lipophilic molecules [4]. Lipid-based systems vary from simple to complex isotropic mixtures of oils, surfactants, and co-surfactant/cosolvents [5]. Apart from enhancing solubility, these systems tend to improve absorption by several auxiliary mechanisms like inhibition of efflux transport mediated by Pglycoprotein, promoting lymphatic transport surpassing the firstpass metabolism and enhancing membrane permeability [6, 7]
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