FORMULATION OPTIMIZATION AND CHARACTERIZATION OF GANCICLOVIR LOADED DRY CHITOSAN NANOPARTICLES

ABSTRACTObjective: The objective of this work was to formulate, optimize, and characterize ganciclovir (GCV) loaded dry chitosan nanoparticles (CSNPs).Methods: The GCV loaded CSNPs was prepared by ionic gelation method. Box–Behnken design was employed to optimize the influence of independentprocess and formulation variables like drug to polymer ratio, concentration of sodium tripolyphosphate, and stirring time (min) on the dependentvariables such as particle size (PS) and drug encapsulation efficiency (% EE). The optimum conditions were determined by regression analysis of theoutput data.Results: The independent variables had interactive effects and they affected both the responses. The optimum formulation had PS within the range of100-120 nm and % EE between 85% and 86%. The prepared GCV loaded CSNPs were dried by fluidized bed drying method. Fourier transform infraredspectra showed there was no physicochemical interaction between GCV and CS. Powder X-ray diffraction study showed less intense crystalline peaksindicated that GCV may exist in the formulation as amorphous nanodispersion or molecular dispersion form. Differential scanning calorimetry studywas performed which indicated that the drug was molecularly dispersed inside the matrix of CS. Higuchi model was the best to fit the in vitro releasedata for the GCV loaded CSNPs.Conclusion: From the results, it can be concluded that the GCV loaded dry CSNPs were formulated, optimized, and characterized using desiredpharmacotechnical properties.Keywords: Chitosan nanoparticles, Box–Behnken design, Sodium tripolyphosphate, Ionic gelation

Mucoadhesive Hydrogel Films of Econazole Nitrate: Formulation and Optimization Using Factorial Design

The mucoadhesive hydrogel film was prepared and optimized for the purpose of local drug delivery to oral cavity for the treatment of oral Candidiasis. The mucoadhesive hydrogel film was prepared with the poly(vinyl alcohol) by freeze/thaw crosslinking technique. 32 full factorial design was employed to optimize the formulation. Number of freeze/thaw cycles (4, 6, and 8 cycles) and the concentration of the poly(vinyl alcohol) (10, 15, and 20%) were used as the independent variables whereas time required for 50% drug release, cumulative percent of drug release at 8th hour, and “k” of zero order equation were used as the dependent variables. The films were evaluated for mucoadhesive strength, in vitro residence time, swelling study, in vitro drug release, and effectiveness against Candida albicans. The concentration of poly(vinyl alcohol) and the number of freeze/thaw cycles both decrease the drug release rate. Mucoadhesive hydrogel film with 15% poly(vinyl alcohol) and 7 freeze/thaw cycles was optimized. The optimized batch exhibited the sustained release of drug and the antifungal studies revealed that the drug released from the film could inhibit the growth of Candida albicans for 12 hours

Formulation, optimization and characterization of cationic polymeric nanoparticles of mast cell stabilizing agent using the Box–Behnken experimental design

<p><i>Objective</i>: The present research work was intended to develop and optimize sustained release of biodegradable chitosan nanoparticles (CSNPs) as delivery vehicle for sodium cromoglicate (SCG) using the circumscribed Box–Behnken experimental design (BBD) and evaluate its potential for oral permeability enhancement.</p> <p><i>Methods</i>: The 3-factor, 3-level BBD was employed to investigate the combined influence of formulation variables on particle size and entrapment efficiency (%EE) of SCG-CSNPs prepared by ionic gelation method. The generated polynomial equation was validated and desirability function was utilized for optimization. Optimized SCG-CSNPs were evaluated for physicochemical, morphological, <i>in-vitro</i> characterizations and permeability enhancement potential by <i>ex-vivo</i> and uptake study using CLSM.</p> <p><i>Results</i>: <i>SCG</i>-CSNPs exhibited particle size of 200.4 ± 4.06 nm and %EE of 62.68 ± 2.4% with unimodal size distribution having cationic, spherical, smooth surface. Physicochemical and <i>in-vitro</i> characterization revealed existence of SCG in amorphous form inside CSNPs without interaction and showed sustained release profile. <i>Ex-vivo</i> and uptake study showed the permeability enhancement potential of CSNPs.</p> <p><i>Conclusions</i>: The developed SCG-CSNPs can be considered as promising delivery strategy with respect to improved permeability and sustained drug release, proving importance of CSNPs as potential oral delivery system for treatment of allergic rhinitis. Hence, further studies should be performed for establishing the pharmacokinetic potential of the CSNPs.</p