FORMULATION, SYSTEMATIC OPTIMIZATION, IN VITRO, EX VIVO, AND STABILITY ASSESSMENT OF TRANSETHOSOME BASED GEL OF CURCUMIN

Objectives: The current work presents a formulation of curcumin-loaded transethosome (CRM-TE) in the form of a gel and its characterization.Methods: Thirteen formulations were prepared by varying the concentration of Phospholipon 90G as lipid, ethanol, and ratio of lipid: Span using Box- Behnken Design. The optimized formulation was characterized by vesicle size, entrapment efficiency, drug retention, drug permeation through skin, and morphology. Parameters of CRM-TE were compared to other vesicular systems that include liposomes, ethosomes, and transfersomes. Optimized CRM-TE was incorporated into gels, and comparative evaluation was performed. CRM-TE gel was kept at 5±3°C, 25±3°C, and 40±3°C for 180 days, further evaluated for entrapment efficacy and vesicle size.Results: CRM-TE showed 286.4 nm vesicle size, 61.2% entrapment efficiency, 19.8% drug retention, and 71.3% drug permeation at 24 h in the skin. It was found superior in terms of all the parameters as compared to other vesicular formulations. CRM-TE gel also exhibited best characteristics in terms of entrapment efficiency, drug retention, and drug permeation. CRM-TE gel exhibited better stability at 5±3°C in terms of vesicle size and entrapment efficiency as compared to other storage conditions.Conclusion: CRM-TE gel could offer efficient delivery of curcumin through topical route

FORMULATION OF CURCUMIN NANOSUSPENSION USING BOX-BEHNKEN DESIGN AND STUDY OF IMPACT OF DRYING TECHNIQUES ON ITS POWDER CHARACTERISTICS

  Objective: The objective of this study was to formulate curcumin nanosuspension (NS) using Box-Behnken design (BBD) and solvent-antisolvent technique to overcome the challenges related to its poor dissolution rate.Methods: Sodium lauryl sulfate (SLS) and poly vinyl pyrrolidone K-60 (PVPK-60) have been used as a surfactant and polymer, respectively, to stabilize the NS. Ethanol was used as solvent to dissolve curcumin and water was used as antisolvent. The study revealed that SLS to curcumin ratio, PVPK-60 to curcumin ratio, solvent to antisolvent ratio and speed of mixing were the critical parameters that affected particle size and zeta potential of the formulation. Hence, based on Box- BBD, 25 formulations were prepared by varying these critical parameters. The optimized batch of CRM NS was further solidified using spray drying as well as rotary evaporation techniques to have a better insight for selection of solidification process in terms of retention of particle size, charge, flow, dissolution, and stability.Results: About 39.47 folds decrease in particle size of raw CRM was observed after conversion into NS. Further, about 53.57 and 45.45 folds decrease in particle size was observed after spray drying and rotary evaporation. Both the dried nanoparticles have shown comparatively higher solubility, powder flow, and dissolution rate as that of raw CRM. Powder X-ray diffraction study revealed the formation of amorphous nanoparticles. Accelerated stability study revealed that nanoparticles dried by spray drying were able to retain the properties such as particle size, flow, and dissolution rate as compared to rotary evaporated powders.Conclusion: It can be concluded that spray drying technique could offer many advantages while loading CRM nanoparticles into tablets for their oral administration