Formulation and Assessment of Celecoxib Floating Beads in Capsule using 2^3 Full Factorial Design

Abstract

Floating beads have been formed to create a prolonged drug release in the stomach and to reduce the number of frequencies, thereby overcoming its side effects. The current study is concerned with the design and evaluation of stomach-specific oil embedded floating beads of celecoxib in a capsule. Hard gelatin capsules (size 1) were filled with celecoxib oil entrapped beads. A 2³ factorial design was used to investigate the effects of different weight masses of HPMC K4M, Sodium alginate, and maize starch on drug encapsulation efficiency (EE) of beads and percent of cumulative drug release at 6 hours (R6h) from capsules. The optimization results show an increase in EE in the oil entrapped beads and a decrease in R6h from capsules with increases in the weights of HPMC K4M, Sodium alginate, and maize starch. The optimized formulation (F6) had EE of 91.80±0.20% and R6h of 37.88±1.39%. The capsules floated over 6 h and released the drug in gastric pH (1.2) during the first two hours then in phosphate buffer pH (6.8) for another four hours. An X-ray imaging in vivo study of optimised capsules containing CXB oil embedded floating beads in rabbits indicated stomachspecific gastro retention throughout a long time. An in vivo anti-inflammatory efficacy of optimized CXB floating beads showed sustained drug release and better inhibition of rats' hind paw edema.

Optimization and In Vitro Characterization of Telmisartan Loaded Sodium Alginate Beads and Its In Vivo Efficacy Investigation in Hypertensive Induced Animal Model

“…The TEL-loaded oil-entrapped floating alginate beads were formulated by emulsion-gelation method using calcium chloride (CaCl 2 ) as a cross-linking agent [ 21 ]. In this method, a sodium alginate solution with various concentrations was prepared by dissolving an accurate amount of sodium alginate in distilled water at room temperature using a magnetic stirrer (Remi Motor, Mumbai, India).…”

“…An accurate amount of TEL (100 mg) was dispersed in sesame oil and mixed with the aqueous solution of sodium alginate in the presence of Tween 80 (0.5%) as an emulsifier by high-shear mixing for 20 min at 2000 rpm using a magnetic stirrer to form an O/W emulsion. The emulsion mixture was extruded into a calcium-chloride solution under mild stirring using a syringe G 21 needle [ 21 ]. The gel beads were allowed to stand in the solution for 15 min to complete the curing reaction and to produce rigid beads.…”

“…The solubility of TEL can be improved by various techniques, such as surface solid dispersions, co-crystals, etc. [ 18 ], whereas formulating it as oil-entrapped beads not only improves solubility but also aids in achieving the sustained activity of the drug [ 19 , 20 , 21 ]. Sodium alginate is used as a polymer to localise and retain the drug in acidic environments; the polymer is selected due to its biocompatibility [ 22 , 23 ], biodegradability, mucoadhesive property [ 24 ], and nontoxicity [ 25 , 26 , 27 ].…”

Statistically-Based Optimization of Verapamil Hydrochloride Loaded Gastroretentive Alginate Beads

“…This might be due to the longer time consumed by high in contrast with previously reported data in literature as it was reported that increasing oil concentration from 15 to 20% w/v would retard drug release (negative effect) because increasing oil would form an additional diffusional barrier for the drug release resulting in slow release of drug from beads 9,39 . Moreover, the drug might stay saturated and distributed in the oil resulting in a drug-oil distributed network 46 .…”