Different Approaches for Enhancement of Curcumin Aqueous Solubility and Dissolution rate

Abstract

Curcumin (CUR) is a nature polyphenolic phytoingredient. CUR showed anti-inflammatory, anti-oxidant, anti-fungal and anticancer activities. The therapeutic efficacy of CUR was limited due to its poor aqueous solubility, poor oral bioavailability. Poor solubility of drugs is the major challenge associated with formulation development. Therefore, the aim of present work was to enhance CUR aqueous solubility and dissolution rate using Physical mixture and its solid dispersion. CUR solid dispersions were prepared by solvent evaporation and Freeze drying techniques using different polymers, such as β-cyclodextrins, polyvinyl pyrrolidone (PVP K30), polyethylene glycol 6000 and Pluronic ® F-127. The prepared physical mixtures, solid dispersions were characterized using different techniques such as (DSC), (FTIR) and (XRD). Furthermore, the solubility and the dissolution rate of the drug in its different systems were explored. The results of physical characterization of the different systems show no interaction between them. Dissolution studies of CUR solid dispersions showed that the highest drug dissolution rate was achieved at CUR/ Pluronic®F-127 weight ratio of 1:3. Also, complete drug dissolution was obtained for CUR/Pluronic F-127 solid dispersion after 30 min compared to 35 % dissolution for CUR alone after the same time. Also, CUR permeability coefficient through rat skin for Pluronic®F-127 micelles and solid dispersion were two times higher than that of the CUR alone. The obtained results concluded that, the preparation of solid dispersion of Pluronic®F-127 solid dispersions by freeze drying method is a promising one to overcome CUR shortcomings through enhancing its aqueous solubility, dissolution rate and skin permeability.

Review: The Chemistry, Toxicity and Antibacterial Activity of Curcumin and Its Analogues

“…Solid dispersion allows for the reduction of drug particle size and crystallinity, increases surface area, and enhances wettability by the surrounding hydrophilic carriers [94][95][96]. Several studies showed that solid dispersion using hydrophilic polymers has significantly enhanced curcumin/analogues solubility and potentially improved their bioavailability and pharmacological potentials [87,[97][98][99][100][101][102][103]. In addition, the encapsulation of curcumin and curcumin analogues in nanoparticles (NPs) has been shown to be feasible and advantageous for overcoming the poor solubility issue and enabling delivery [56].…”

“…The clinical use of curcumin/analogues was hindered by their hydrophobic nature and poor solubility in water, which negatively affected their bioavailability and pharmacological potentials [48]. The complexation of curcumin/analogues with various host compounds has been shown to be successful, with significantly increased solubility and bioavailability when using cyclodextrin [85][86][87][88][89], modified rice starch and polysaccharide complexes [90], pea protein [91], starch, and gelatine [92], as well as whey protein [91,93]. Solid dispersion approach has also been used to enhance the drug dissolution rate and solubility.…”

In- Vitro Evaluation of Nanocurcumin Against Multi-Drug Resistant Bacteria

“…Weighed amount of nanocurcumin and their physical mixtures were placed in dissolution medium that consists of 500 ml of phosphate buffer pH 7.4 contains Tween 80 (0.1 % w/v) to maintain sink condition. Dissolution system was kept at 37 °C and agitated at constant rate of 50 rpm 19 . At specified time intervals of 5, 15, 30, 60, 90, and 120 minutes, aliquots of 5 mL were withdrawn and filtered by membrane disc filter (0.45µm).…”