Nanoemulsion: for improved oral delivery of repaglinide

Abstract

Repaglinide (RPG) is a fast-acting prandial glucose regulator. It acts by stimulating insulin release from pancreatic b-cells. Recurrent dosing of RPG before each meal is burdensome remedy. Hence the plan of the present study was to evaluate nanoemulsion as a hopeful carrier for RPG for persistent hypoglycemic effect. The drug was incorporated into oil phase of nanoemulsion to give improved biopharmaceutical properties as compared to the lipid-based systems. Pseudo ternary phase diagrams were prepared by aqueous titration method. Formulations were selected at a difference of 5% w/w of oil from the o/w nanoemulsion region of phase diagrams. The optimized nanoemulsion formulation constituted sefsol-218 (5% v/v) as an oil phase, 30% v/v of Tween-80 and transcutol as a surfactant and co-surfactant to restrain nanodroplet size and low viscosity and distilled water (65%). In vitro dissolution studies showed higher drug release (98.22%), finest droplet size (76.23 nm), slightest polydispersity value (0.183), least viscosity (21.45 cps) and immeasurable dilution capability from the nanoemulsion as compared with existing oral tablet formulation. The optimized RPG nanoemulsion formulation showed better hypoglycemic effect in comparison to tablet formulation in experimental diabetic rats. No significant variations were also observed in the optimized formulation when subjected to accelerated stability study at different temperature and relative humidity over a period of 3 months.

Silymarin nanoemulsion against human hepatocellular carcinoma: development and optimization

“…It offers a promising solution to many difficulties in drug delivery and tissue engineering [8], a nano-sized drug vehicle has made significant progress in the delivery of conventionally undeliverable molecules, such as compounds with low water solubility and genetic biomolecules [9,10]. The newer formulation design approaches for bioavailability enhancement includes incorporation of the active component into inert lipid vehicles [11], such as oils [12], surfactant dispersions [13][14][15], self-emulsifying formulations [16,17], emulsions [18][19][20][21], micro or nanoemulsions [22][23][24], and liposomes [25]. Nanoemulsion offers several advantages over these drug delivery systems like higher solubilisation capacity, rapid onset of action (no extra time for dispersion), reduced intersubject variability in terms of gastrointestinal fluid volume and longer shelf life [26], and toxicological safety, a high content of the lipid phase and the possibility of large-scale production by high-pressure homogenization [27].…”

Cross-Linked Polymer-Stabilized Nanocomposites for the Treatment of Bacterial Biofilms

“…We hypothesized that using a polymer-stabilized essential oil platform would enable us to generate nano-sized emulsions to improve the delivery of the payload, 31 and to increase its stability 32 by incorporating crosslinking strategies. Herein, we report an essential oil-in-water crosslinked polymer nanocomposite (X-NC) for the treatment of bacterial biofilms (Scheme 1).…”

Nanoemulsion-based delivery system for enhanced oral bioavailability and Caco-2 cell monolayers permeability of berberine hydrochloride

“…Nanoemulsion is a thermodynamically stable system and transparent dispersions of oil and water with the droplet size less than 100 nm stabilized by an interfacial film of surfactant molecules. In recent years, nanoemulsions has become a promising approach for the delivery of poorly water-soluble drugs to improve oral bioavailability as well as to modify drug release characteristics (Aboalnaja et al, 2016;Akhtar et al, 2016;Khani et al, 2016). The mechanisms for enhanced absorption of nanoemulsions are very complex, involving improved solubility of drug molecules, formation of mixed micelles, opening of tight junctions, and improved lymphatic delivery (Qi et al, 2011;Aboalnaja et al, 2016).…”