Formulation and Optimization of Curcumin Solid Dispersion Pellets for Improved Solubility

Abstract

Objective: The present study was aimed at designing of solid dispersion based pellets of curcumin (Cu) for improving its solubility.
 Methods: Solid dispersion (SD) of Cu was prepared by the melt method using Poloxamer 407 (Pol 407) at a different weight ratio of Cu-Pol 407 (1:2, 1:3, 1:5, 1:7, 1:10). The solid dispersion was characterised by FTIR, SEM, DSC, XRD and evaluated for saturation solubility in water, drug content and in vitro dissolution. The pellets of Cu solid dispersion were prepared by extrusion spheronization technique and optimization was performed by 32full factorial design. The pellets were evaluated for size distribution, flow properties, hardness, disintegration and in vitro drug dissolution.
 Results: From the phase solubility analysis, Pol 407 was selected as a Solid dispersion carrier. The formation of Cu-SD by melt method using Pol 407, was confirmed from FTIR and DSC studies. XRD studies indicated a change of Cu from crystalline to amorphous form. There was a significant increase of Cu when formulated as SD compared to plain Cu. The optimization of extrusion spheronization process revealed the significant effect of Cu-Pol 407 ratio (p<0.0001) on in vitro dissolution of pellets. Higher Cu dissolution was obtained with Cu-SD pellets compared to plain Cu pellets.
 Conclusion: The present study demonstrated the potential of Cu-SD pellets in improving the solubility of poorly soluble Cu.

Quality aspects in the development of pelletized dosage forms

“…The most preferable processing can be done at temperature above the M.P. of semi-crystalline polymers or [ 50 , 51 , 52 , 53 , 54 , 55 , 56 , 57 , 58 , 59 , 60 , 61 , 62 , 63 , 64 , 65 , 66 , 67 , 68 , 69 , 70 , 71 , 72 , 73 , 74 , 75 , 76 , 77 , 78 , 79 , 80 , 81 , 82 , 83 , 84 , 85 , 86 , 87 , 88 , 89 , 90 , 91 , 92 , 93 , 94 , 95 , 96 , 97 , 98 , 99 , 100 ] °C above the glass transition temperature Tg of amorphous polymers, but below the M. P. of the crystalline API [ 80 , 81 ].…”

“…The solid dispersion of curcumin using different ratio of Poloxamer 407 by melt method were finally extruded and spheronize. The resulting pellets showed increase in solubilisation however it is noteworthy that pelletization process had no impact on solubilisation of solid dispersion [ 94 ], were formulated as pellets without any impact on drug release profile.…”

Formulation and Evaluation of Sustained-Release Pellets of Lornoxicam

“…SEM photomicrograph of pellets revealed that the pellets were spherical shaped in nature and the surface was rough. This could be due to the deposition of fines produced by attrition of pellets during spheronization [26] [fig. 9].…”

An Outline of Variables in Pelletization by Extrusion and Spheronization

“…Delayed-release pellets of omeprazole magnesium, which is unstable in stomach pH, hence formulated as delayed-release dosage form to allow absorption in intestinal pH [38]. Deshkar et al, designed curcumin solid dispersion pellets for improving the solubility of poorly soluble curcumin and observed a significant enhancement in dissolution compared to pure curcumin pellets [39]. Fielden et al, reported that particle size of lactose powder ( fine and coarse) has an effect on the extrusion characteristics of the wet mass and on the size and the roundness of the resulting pellets when prepared using cylinder extruder and a ram extruder [40].…”