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The objective of this work was to prepare and optimize the fast-dissolving film of salbutamol sulphate, which can be useful in an acute attack of asthma. The film was prepared using a solvent evaporation technique and is taken through the sublingual route. The film contains polyvinyl alcohol as a polymer, glycerol as a plasticizer, and mannitol as filler. A 33 full factorial design was utilized for the optimization of the effect of independent variables such as amount of polyvinyl alcohol, amount of glycerol, amount of mannitol on the mechanical properties, and % drug release of film. The multiple regression analysis of the results led to equations that adequately describe the influence of the independent variables on the selected responses. Polynomial regression equations and contour plots were used to relate the dependent and independent variables. The experimental results indicated that polymer concentration, plasticizer concentration, and filler concentration had complex effects on film mechanical behavior and % drug release. Furthermore, the desirability function was employed in order to determine the best batch out of all 27 batches of the factorial design. The % relative error was calculated, which showed that observed responses were in close agreement with the predicted values calculated from the generated regression equations. It was found that the optimum values of the responses for fast release film could be obtained at medium levels of polyvinyl alcohol and glycerol, and a high level of mannitol. The prepared film was clear, transparent, and had a smooth surface. The concept of similarity factors Sd was used to prove similarity of dissolution between distilled water and simulated saliva (pH 6.8) or simulated gastric fluid (pH 1.2).

Abstract. The purpose of this work was to design and optimize a novel vaginal drug delivery system for more effective treatment against vaginal candidiasis. Itraconazole was formulated in bioadhesive film formulations that could be retained in the vagina for prolonged intervals. The polymeric films were prepared by solvent evaporation and optimized for various physicodynamic and aesthetic properties. In addition, percentage drug retained on vaginal mucosa was evaluated using a simulated dynamic vaginal system as function of time. A polymeric film containing 100 mg itraconazole per unit (2.5 cm×2.5 cm) have been developed using generally regarded as safe listed excipients. The pH of vaginal film was found to be slightly acidic (4.90±0.04) in simulated vaginal fluid and alkaline (7.04±0.07) in water. The little moisture content (7.66±0.51% w/w) was present in the film, which helps them to remain stable and kept them from being completely dry and brittle. The mechanical properties, tensile strength, and percentage elongation at break (9.64 N/mm 2 and 67.56% for ITRF 65 ) reveal that the formulations were found to be soft and tough. The films (ITRF 65 ) contained solid dispersion of itraconazole (2.5)/hydroxypropyl cellulose (1)/polyethylene glycol 400 (0.5), which was found to be the optimal composition for a novel bioadhesive vaginal formulation, as they showed good peelability, relatively good swelling index, and moderate tensile strength and retained vaginal mucosa up to 8 h. Also, the film did not markedly affect normal vaginal flora (lactobacillus) and was noncytotoxic as indicated by the negligible decrease in cell viability.

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This work examines the influence of various process parameters (like sodium alginate concentration, calcium chloride concentration, and hardening time) on papain entrapped in ionotropically cross-linked alginate beads for stability improvement and site-specific delivery to the small intestine using neural network modeling. A 3(3) full-factorial design and feed-forward neural network with multilayer perceptron was used to investigate the effect of process variables on percentage of entrapment, time required for 50% and 90% of the enzyme release, particle size, and angle of repose. Topographical characterization was conducted by scanning electron microscopy, and entrapment was confirmed by Fourier transform infrared spectroscopy and differential scanning calorimetry. Times required for 50% (T(50)) and 90% (T(90)) of enzyme release were increased in all 3 of the process variables. Percentage entrapment and particle size were found to be directly proportional to sodium alginate concentration and inversely proportional to calcium chloride concentration and hardening time, whereas angle of repose and degree of cross-linking showed exactly opposite proportionality. Beads with >90% entrapment and T(50) of <10 minutes could be obtained at the low levels of all 3 of the process variables. The inability of beads to dissolve in acidic environment, with complete dissolution in buffer of pH >or=6.8, showed the suitability of beads to release papain into the small intestine. The shelf-life of the capsules prepared using the papain-loaded alginate beads was found to be 3.60 years compared with 1.01 years of the marketed formulation. It can be inferred from the above results that the proposed methodology can be used to prepare papain-loaded alginate beads for stability improvement and site-specific delivery.

The objective of this work was to study dissolution enhancement efficiency and solid dispersion formation ability of hydrophilic swellable polymers such as sodium carboxymethyl cellulose (Na-CMC), sodium starch glycolate (SSG), pregelatinized starch (PGS), and hydroxypropylmethyl cellulose (HPMC) with carbamazepine using 3 2 full factorial design for each of the polymers. Solid dispersions of carbamazepine were prepared using solvent evaporation method with around 70% solvent recovery. The independent variables were the amount of polymer and organic solvent. The dependent variables assessed were percentage drug dissolved at various time points and dispersion efficiency (ie, in terms of particle size of solid dispersion). Solid dispersions were evaluated for percentage drug dissolved, wettability, differential scanning calorimetry, scanning electron microscopy, and angle of repose. Multiple linear regression of results obtained led to equations, which generated contour plots to relate the dependent variables. Similarity factor and mean dissolution time were used to compare dissolution patterns obtained in distilled water and simulated gastric fluid United States Pharmacopeia (USP) XXVI of pH 1.2. Maximum drug dissolution was obtained with polymer order Na-CMC9SSG9PGS9HPMC. Particle size of drug was reduced~10-15, 3-5, 5-7, and 10-25 times in Na-CMC, SSG, PGS, and HPMC solid dispersions, respectively; whereas wettability of solid dispersions was found in the order of Na-CMC9HPMC9PGS9SSG. Angle of repose was found to be in the range of 29°to 35°for all solid dispersions, which shows good flowability characteristics. HPMC showed increase in drug dissolution up to an optimized level; however, further increase in its concentration decreased drug dissolution.

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