Abstract
Objective: Emulsomes are novel vesicular drug delivery system with an internal solid lipid core surrounded by one or more bilayers of phospholipids. Etodolac is a potent anti-inflammatory drug and is a drug of choice for the treatment of various diseases. The present study is focused on the development of emulsomes using etodolac as drug candidates having improved drug loading with sustained-release effect for patient compliance.
 Methods: Emulsomes formulation composed of solid lipids (tristearin), phospholipids, cholesterol, stearylamine, and drug (etodolac) were prepared by lipid film hydration method followed by sonication to produce emulsomes of the nanometric size range. All the formulations were optimized by using box-behnken design of experiment considering 3 factors viz. drug to phospholipid ratio (A), tristearin to phospholipid ratio (B), stearylamine to phospholipid ratio (C) at 3 levels lower (-1), middle (0) and upper (+1). The response of the independent variables (A, B, C) was studied on the dependent variable viz. particle size (Y1), zeta potential (Y2), and entrapment efficiency (Y3). The responses were analyzed by design expert software to find out the optimized values of variables within the design space.
 Results: Compatibility with excipients was established by FTIR studies. The developed emulsomes were spherical shape vesicles as analyzed by TEM. The optimized batch (OB) was evaluated for particle size, zeta potential, and entrapment efficiency with experimental values 383.1 ± 11.7 nm, 47.2 ± 1.3 mV and 80.1 ± 3.2% and predicted values 390.394 nm, 45.000 mV and 81.642 %, respectively. The experimental values were found in reasonable agreement with predicted values by the design of the experiment. In vitro drug release study showed sustained release of the drug (88.69 % after 24 h).
 Conclusion: Etodolac loaded emulsomes is a novel drug delivery system and found to reliable in terms of various characteristic parameters like particle size, zeta potential, entrapment efficiency, and drug release. 3-factors 3-levels Box-behnken design of the experiment is a suitable design for the optimization of emulsomes.
Highlights
Lipid-based drug delivery systems have gained the attention of researchers in the recent few decades due to their certain advantages over other drug delivery systems
Etodolac was procured from Balaji chemicals Surat, tristearin, and lecithin were procured from HiMedia, cholesterol was procured from LOBA chemie Mumbai, sephadex G-50 was procured from Sigma aldrich USA, stearylamine was procured from Ottokemi, Mumbai
All the 17 batches were prepared and their responses were recorded as shown in table 2. It was observed from the responses obtained that independent variables (A, B, C) have a significant effect on the dependent variables
Summary
Lipid-based drug delivery systems have gained the attention of researchers in the recent few decades due to their certain advantages over other drug delivery systems. Emulsomes have been proven to be advantageous for the delivery of lipophillic drugs. Emulsomes is a lipid-based, vesicular drug delivery carrier having structurally similarity with liposomes but differs only in core component as emulsomes unlike liposomes is composed of solid core [3]. This system becomes advantageous as a carrier system for lipophillic drugs having high drug entrapped by encapsulating lipophillic drugs in lipid core as well as between phospholipid bilayers [6]. Drug entrapped in solid lipid core exhibits sustained release [7]. Emulsomes may be considered as an efficient drug delivery system because of biocompatibility, biodegradability, stability in the gastrointestinal tract, high entrapment efficiency, and sustained drug release [10, 11]
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