Formulation of Curcumin Nanosuspension Using Box-Behnken Design and Study of Impact of Drying Techniques on Its Powder Characteristics

Abstract

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.

Novel Therapeutic Delivery of Nanocurcumin in Central Nervous System Related Disorders

“…Curcumin solid lipid nanoparticles (Cur-SLNs) formulate with P-gp modulator excipients, TPGS (D-α-Tocopherol polyethylene glycol 1000 succinate) and Brij78 (that is a docosaethylene glycol mono octadecyl ether), enhance the solubility and bioavailability of curcumin. Again, curcumin nanosuspension prepared by precipitation method with sodium lauryl sulphate and polyvinylpyrrolidone k-60 showed an increased oral solubility, stability and dissolution rate with respect to pure curcumin [ 153 ]. High speed homogenization for the nanosuspension formulation by using Arabic gum as a natural polymeric surfactant was reported [ 154 ].…”

Enhancement of the Release of Curcumin by the Freeze Drying Technique Using Inulin and Neusilin as Carriers

“…As consequence of its low solubility, CUR exhibits poor dissolution and bioavailability properties limiting its clinical use and enlarging the administered dose to 8-12g daily. Despite of the high administered dose, CUR plasma concentration was less than 1 µg/ml and this concentration has no therapeutic activity [8][9][10]. CUR structure present in fig.…”

“…One of the most promising techniques to improve CUR solubility is preparing it in the amorphous form by freeze drying [10,16]. It is well known that the amorphous form has higher aqueous solubility and dissolution characteristics than the corresponding crystal form.…”

“…The main drawback of this method is the physical instability due recrystallization. Several additives have been used to stabilize the amorphous form of CUR such as Maltodextrin [17],PVP [10], HPMC [16], Gelucire-Aerosol combination [18]. The use of such additives showed some enhancement in stability.…”