Product Development Studies on Surface-Adsorbed Nanoemulsion of Olmesartan Medoxomil as a Capsular Dosage Form

Abstract

Abstract. The present study aimed at development of capsular dosage form of surface-adsorbed nanoemulsion (NE) of olmesartan medoxomil (OLM) so as to overcome the limitations associated with handling of liquid NEs without affecting their pharmaceutical efficacy. Selection of oil, surfactant, and cosurfactant for construction of pseudoternary phase diagrams was made on the basis of solubility of drug in these excipients. Rationally selected NE formulations were evaluated for percentage transmittance, viscosity, refractive index, globule size, zeta potential, and polydispersity index (PDI). Formulation (F3) comprising of Capmul MCM® (10% v/v), Tween 80® (11.25% v/v), polyethylene glycol 400 (3.75% v/v), and double-distilled water (75% v/v) displayed highest percentage cumulative drug release (%CDR; 96.69± 1.841), least globule size (17.51±5.87 nm), low PDI (0.203±0.032), high zeta potential (−58.93±0.98 mV), and hence was selected as the optimized formulation. F3 was adsorbed over colloidal silicon dioxide (2 ml/400 mg) to produce free-flowing solid surface-adsorbed NE that presented a ready-to-fill capsule composition. Conversion of NE to surface-adsorbed NE and its reconstitution to NE did not affect the in vitro release profile of OLM as the similarity factor with respect to NE was found to be 66% and 73% respectively. The %CDR after 12 h for optimized NE, surface-adsorbed NE, and reconstituted NE was found to be 96.69±0.54, 96.07±1.76, and 94.78±1.57, respectively (p>0.05). The present study established capsulated surfaceadsorbed NE as a viable delivery system with the potential to overcome the handling limitations of NE.

Limonene-based Self-nanoemulsifying System: Formulation, Physicochemical Characterization and Stability

“…The selected formulation was visually assessed and classified accordingly to the following criteria; rapidly forming emulsion having a clear or bluish appearance (grade A), rapidly forming, slightly less clear emulsion, having a bluish white appearance (grade B), fine milky emulsion formed within two minutes (grade C), dull, greyish white emulsion having slightly oily appearance that is slow to emulsify longer than two minutes (grade D), or poor minimal emulsification with large oil globules present on the surface (grade E). 15 In order to determine the formulation the cloud point, the prepared formulation was diluted with deionized water in ratio of 1:100 then placed in a water-bath (FALC, WB-MF24, Treviglio (BG) -Italy) with gradual increase in the temperature at a rate of 1°C/ min. At the cloud point, the drop in sample percentage transmittance was measured spectrophotometrically at 638.2 nm.…”

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“…Therefore, water was used as a dispersion medium to simulate the emulsification efficiency of SNEDDS upon infinite dilution in GI fluids 12 .…”

“…Drugs that are substrates for P-gp bind and are transported back to the apical surface of the tissue in an ATPdependent manner, thereby restricting the overall permeability of drugs. Cremophor ® EL, and Tween ® 80 were used to inhibit P-gp efflux transporter activity in Caco-2 cell monolayers of the intestinal mucosa 12,20 .…”

“…The supernatant was taken and filtered through a cellulose acetate membrane filter (0.45µm) 21 . The concentration of OLM was determined spectrophotometrically at 257nm after appropriate dilution 12,22 . Characterization of OLM-Loaded SNEDDS: Determination of the Emulsification Time: A predetermined weight (1gm) of each system was introduced into 200mL of distilled water maintained at 37 ± 0.5 °C in a glass beaker and the contents were mixed gently using a magnetic stirrer rotating at constant speed (100 rpm) 23 .…”

Design, Optimization and in Vitro Characterization of Self Nano Emulsifying Drug Delivery System of Olmesartan Medoxomil

“…Experiments were run in random order to increase the predictability of the model. Optimisation was performed using a desirability function to obtain the levels of X1, X2 and X3, which minimised (Y1) and (Y3) and maximised (Y2) [16][17][18][19][20][21]. The quadratic model generated by design is as follows:…”