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In current study, a nanoemulsion as drug delivery system (NE) of spray dried Boswellia Serrata Extract (BSE) was developed and characterized to compare it in vitro/Ex vivo diffusion with reference formulation. Pseudo-ternary phase diagrams were constructed by phase diagram by aqueous titration method, of which the evaluation method was improved for solubility, Droplet size and transmittance. The formulation of BSE-loaded NE was optimized by a Simplex lattice mixture experimental design. The optimized nanoemulsion formulation, loading with 199.8 mg g-1 BSE total boswellic acids, consisted of Isopropyl Myristate, Tween 80 and Ethanol (2:8:10, w/w) and it remained stable after storing at 40°C, 25°C, 4°C for at least 6 months. When diluted with water, the NE droplet size was 11.25 nm and the zeta potential was 0.223 mV. The spherical droplet shape was confirmed by TEM analysis. Ex vivo skin permeation and in vivo anti-inflammatory study were conducted. About 3.25 fold increase in flux was seen in case of nanoemulsion, nanogel showed 1.45 fold increase in flux as compared to carbopol gel with highest enhancement ratio 4.57 and 1.59 respectively. Our study illustrated potential of developed nanoemulsion as possible alternative to traditional topical formulations.

The drug-excipient compatibility study of quetiapine fumarate, with widely used sustained release excipients, was carried out employing differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR). The selected excipients were HPMC K100M, sodium alginate, xanthan gum, Eudragit RSPO, hydrogenated castor oil, carnauba wax, and PEO WSR 303. Equal proportion of drug and excipients was utilized in the interaction study. FT-IR spectra indicated the absence of interaction between drug and excipients. The DSC curve showed a sharp endothermic melting peak at 173.26 °C for quetiapine fumarate. Post melting interaction was observed for carnauba wax, Eudragit RSPO, and hydrogenated castor oil probably due to solubilization of drug in the melted excipient. No interaction was observed for other excipients. The physical mixtures stored at 30 ± 2 °C/65 ± 5% RH did not show any significant degradation of the drug. The concept of systemically conducted preformulation studies will facilitate dossier submission to the drug control authority.

Context: Transdermal spray (TS) of clotrimazole (CTZ) was formulated to improve the drug transport through the skin up to 12 h to achieve the antifungal efficacy. Objective: The aim of present study was to formulate and evaluate antifungal transdermal spray to improve the permeation of clotrimazole across the skin and to decrease the dosing frequency in fungal infection. Materials and methods: Different ratios of ethanol and acetone and various grades of eudragit and ethyl cellulose were evaluated according to six criteria: viscosity, drying time, stickiness, appearance and integrity on skin and water washability. Propylene glycol (PG) and polyethylene glycol 400 (PEG 400) were used in the study as plasticizer and solubilizer. The TS was evaluated for in vitro drug release, spray angle, spray pattern, average weight per dose, pH, drug content, evaporation time, leak test and antifungal efficacy study. Results and discussion: Eudragit E100 and blend of ethanol and acetone (80:20) satisfied the desired criteria. The selection of optimized batch was based on the results of in vitro drug release, spray pattern and spray angle. The optimized batch showed the spray angle Conclusion: The TS of CTZ can be an innovative and promising approach for the topical administration in the fungal diseases.

A co-grinding method was used to improve the dissolution characteristics of nimesulide, a poorly water-soluble non-steroidal anti-inflammatory drug. Nimesulide solubility was studied to determine the solubilization process using different concentrations of Tween 80 at different pH values. At a 10% Tween 80 concentration, a large proportion (> 90%) of drug was entrapped in micelles when the pH of buffer solution was greater than pKa of nimesulide. A 32 factorial design was adopted using the concentration of Tween 80 and sodium lauryl sulphate as independent variables. Improved drug dissolution was obtained when the drug was mixed first with aqueous surfactant solution and later blended with adjuvant such as lactose and microcrystalline cellulose. Sodium lauryl sulphate was more effective in increasing the drug dissolution compared with Tween 80. The use of a blend of Tween 80 and sodium lauryl sulphate is justified since the interaction term (Tween 80 x sodium lauryl sulphate) for percentage drug release in 45 and 120 min was not significant. Contour plots were obtained for the angle of repose and percentage drug release in 30, 45 and 120 min. The study revealed that optimum level of surfactants should be used. The granule flow was adversely affected and no further improvement of drug dissolution was observed when the surfactants were used at high levels. The improved drug dissolution may be attributed to improved wetting and micellization due to presence of surfactants or hydrophilic adjuvant. More than two-fold increase in the drug dissolution was obtained by the selected batches.

The purpose of this study was to develop sustained-release tablets of diltiazem HCl using alkali-treated guar gum as a hydrophilic matrixing agent. The effect of NaOH concentration on swelling of modified guar gum was more pronounced than that of time and temperature. The tablets of diltiazem HCl, containing either untreated or modified guar gum, were compared in terms of drug dissolution, matrix erosion and hydration. The drug release profile of the tablets containing untreated guar gum showed a tailing effect in the terminal phase, which was not observed in the tablets containing modified guar gum. Poor correlation was found between erosion and drug dissolution. The tablets swelled considerably during the hydration study. A uniform precision rotatable central composite design was used to investigate the influence of the amount of diltiazem HCl, modified guar gum and succinic acid on in-vitro drug dissolution. Interactive polynomial models were evolved for the time required for 63.2(t63.2) and 80% (t80) drug release. Response surface plots were generated to show the effect of formulation variables on t63.2. A polynomial equation was also derived for prediction of the drug release profile. An ideal formulation was selected by applying various constraints such as t63.2, t80 and percentage drug released in 60, 360, 540 and 720 min. The kinetics of drug release fitted the Weibull model. It was concluded that modified guar gum could be used as an economical hydrophilic matrixing agent for the formulation of sustained-release tablets of diltiazem HCl.

The present study deals with the preparation of microspheres of diclofenac sodium using cross-linked poly(vinyl alcohol) (PVA). A central composite design consisting of a two-level full factorial design superimposed on a star design was employed for developing the microspheres. The PVA to the drug ratio X1 and amount of glutaral-dehyde cross-linking agent X2 were chosen as the independent variables. The time required for 50% drug dissolution t50 in phosphate buffer (pH 7.2) was selected as the dependent variable. An optimum polynomial equation was generated for the prediction of the response variable t50. Based on the results of multiple linear regression analysis and F statistics, it may be concluded that sustained action can be obtained when X1 and X2 are kept at high levels. The X1X2 interaction was found to be statistically significant. A response surface plot is presented to show the effects of X1 and X2 on t50. The drug release pattern fit the Higuchi model well. A model was validated for accurate prediction of the drug dissolution profile with constraints on the percentage drug release in the first, fifth, and seventh hours. The data of a selected batch were subjected to an optimization study, and an optimal formulation was fabricated. Good agreement was observed between the predicted and the observed dissolution profiles of the optimal formulation.

Seven batches of poly(D, L-lactic acid) (PLA) were prepared from D, L-lactic acid using tetraphenyltin or zinc acetate as a catalyst. The samples of PLA were characterized by terminal group analysis, gel permeation chromatography, infrared analysis, and differential scanning calorimetry. Polymerization conditions such as the time of reaction and the type of catalyst affected the molecular weight of PLA. Microspheres containing indomethacin were prepared by the oil/water (o/w) solvent evaporation technique using different formulations and process variables. The in vitro release of indornethacin in phosphate buffer was found to be dependent on the molecular weight of PLA and also on the type and amount of adjuvants used. The batch of microspheres containing 5% cholesterol released the drug at a slow controlled rate (29%, 65%. and 85% in 1, 7, and 24 hr, respectively). The results of F test for the microspheres revealed that there is no significant direrence between the Higuchi model and the power la...

Ethyl cellulose pseudolatices were prepared by an emulsion-solvent evaporation technique, which consisted of dissolving the polymer in a blend of benzene and ethyl alcohol, followed by the addition of adjuvants. The organic, solvents were removed from the emulsion using vacuum distillation. Physical evaluation of the dispersions and the cast films was carried out.On the basis of characteristics of cast films selected formulations were fused as granulating agents for preparing chlorpheniramine maleate tablets. Good correlation was observed between total solid in the granulating dispersion and the drug release. The possible mechanisms for the drug release from the tablets are suggested.

The objective of this study was to develop modified-release tablets of diltiazem HCl using a direct compression technique. A 3(2) factorial design was employed using the amount of alkali-treated guar gum and cetyl alcohol as independent variables. This article proposes the use of a novel approach-f2 and Sd values as dependent variables-to evaluate the effect of selected independent variables along with other dependent variables (i.e., percentage drug released in x min, Yx; time required for z% drug release, tz; and mean dissolution time (MDT)). It is concluded that when a decision is to be made for the selection of a best batch, it is perhaps more realistic to use the f2 or Sd value which takes into account the dissolution profile as a whole, as opposed to Yx and tz values which use just one point from the dissolution plot. The batch showing the f2 value nearest to 100 or the Sd value nearest to zero is ranked as the best batch (diltiazem HCl 90 mg, alkali-treated guar gum 80 mg and cetyl alcohol 15 mg). The gel strength and matrix erosion of the formulated tablets were dependent on the type and amount of the adjuvants. The drug release rate is well correlated with matrix erosion. The kinetics of drug release fitted best to the Korsmeyer and Peppas model. It is concluded that by using a proper combination of the hydrophilic polymer and cetyl alcohol one can achieve a desirable drug release pattern.

The aim of the present investigation was to develop oral films of valdecoxib using Eudragit EPO and hydroxypropylmethylcellulose. Films of Eudragit EPO, hydroxypropylmethylcellulose and Eudragit EPO combined with hydroxypropylmethylcellulose were prepared by film casting method. Glycerol, menthol and aspartame were incorporated in the drug containing films as plasticizer, cooling agent and sweetener, respectively. The drug loading was 10 mg valdecoxib per 4 cm2 of the film. The films were evaluated for hydration study, folding endurance and in vitro drug dissolution in the distilled water. The films containing both Eudragit EPO and hydroxypropylmethylcellulose films showed neutral surface pH when prepared using 0.1 N HCl as a solvent. Glycerol played a critical role in imparting flexibility to the film and improving the drug release from film. The bitter taste of the drug was masked by using aspartame and menthol accompanied by the synergistic effect of Eudragit and glycerol. Water uptake by films was found to be dependant both on the amount of Eudragit EPO and glycerol. The films containing the higher proportion of glycerol showed higher water uptake and faster drug release at all the sampling time in the in vitro dissolution test. Optimum plasticity was obtained using the required concentration of hydroxypropylmethylcellulose and glycerol. The study revealed that taste masked valdecoxib films can be developed by the selection of appropriate film former and by the use of auxiliary excipients.

Withaferin A, a steroidal lactone which is present in dry root extract of Withania somnifera (WSE), is reported to possess numerous pharmacological activities and shows poor aqueous solubility. The purpose of this study is to enhance the dissolution rate and oral bioavailability of WSE by incorporating it in self nano emulsifying drug delivery system (SNEDDS). Capmul MCM-based SNEDDS formulation with Tween 20 as surfactant and ethanol as co surfactant was developed for oral delivery of withaferin A. Optimised SNEDDS was evaluated for its self-emulsification time and viscosity, droplet size. The optimised SNEDDS formulation containing withaferin A, Capmul MCM(12.4%), Tween 20 (58.2%) and ethanol (29%), and showed higher in vitro drug release as compared to pure WSE. These results demonstrate the potential use of SNEDDS for improving the oral bioavailability of poor water soluble compounds such as withaferin A.

Ratio derivative spectrophotometric method has been developed for the simultaneous determination of artemisinin and curcumin. The overlapping spectra of both drugs were resolved by making use of the first-derivative of the ratios of their direct absorption spectra. The derivative ratio absorbances of artemisinin and curcumin were measured at λmax 293.17 and λmax 457.0 nm, respectively, for their quantification. Artemisinin and curcumin were determined in the concentration range of 2-10 μg/mL and 1-5 μg/mL, respectively. The method was validated as per the ICH guidelines and accuracy, precision were found to be within acceptable limit. The limits of detection and quantitation were found to be 0.003299 and 0.009997 μg/mL, respectively for artemisinin and 0.006743 and 0.020434 μg/mL, respectively for curcumin. The proposed ratio first derivative spectrophotometric method is novel, rapid, simple, sensitive, accurate, precise and successfully applicable for simultaneous estimation of artemisinin and curcumin in parentral dosage form.