Preparation of Curcumin-Loaded Liposomes and Evaluation of Their Skin Permeation and Pharmacodynamics

Abstract

This study aimed to investigate the in vitro skin permeation and in vivo antineoplastic effect of curcumin by using liposomes as the transdermal drug-delivery system. Soybean phospholipids (SPC), egg yolk phospholipids (EPC), and hydrogenated soybean phospholipids (HSPC) were selected for the preparation of different kinds of phospholipids composed of curcumin-loaded liposomes: C-SPC-L (curcumin-loaded SPC liposomes), C-EPC-L (curcumin-loaded EPC liposomes), and C-HSPC-L (curcumin-loaded HSPC liposomes). The physical properties of different lipsomes were investigated as follows: photon correlation spectroscopy revealed that the average particle sizes of the three types of curcumin-loaded liposomes were 82.37 ± 2.19 nm (C-SPC-L), 83.13 ± 4.89 nm (C-EPC-L), and 92.42 ± 4.56 nm (C-HSPC-L), respectively. The encapsulation efficiency values were found to be 82.32 ± 3.91%, 81.59 ± 2.38%, and 80.77 ± 4.12%, respectively. An in vitro skin penetration study indicated that C-SPC-L most significantly promoted drug permeation and deposition followed by C-EPC-L, C-HSPC-L, and curcumin solution. Moreover, C-SPC-L displayed the greatest ability of all loaded liposomes to inhibit the growth of B16BL6 melanoma cells. Therefore, the C-SPC-L were chosen for further pharmacodynamic evaluation. A significant effect on antimelanoma activity was observed with C-SPC-L, as compared to treatment with curcumin solution in vivo. These results suggest that C-SPC-L would be a promising transdermal carrier for curcumin in cancer treatment.

Influence of Lipid Composition, pH, and Temperature on Physicochemical Properties of Liposomes with Curcumin as Model Drug

“…Faster diffusion of curcumin without liposomes compared to that embedded in liposomes demonstrates the sustained release of entrapped curcumin. Thus, liposomes can act as effective drug delivery systems, ensuring the sustained and prolonged release of curcumin 38,65 . Initially, a burst release was recorded for curcumin in all formulations which occurred because of the release of curcumin adsorbed on the liposome surface as well as the free curcumin molecules.…”

“…A dialysis bag 12 kDa molecular weight cut-off, Sigma-Aldrich was used. While the donor medium contained 5 mL curcumin-loaded liposomes or aqueous curcumin solution control , the receptor compartment contained 20 mL phosphate-buffered saline buffer pH 7.4 with 0.5 Tween-80 and 20 ethanol v/v as a sink at 37 38 . At specific time intervals, 3 mL receptor medium was withdrawn with concomitant addition of the same volume of fresh medium and the aliquots were analyzed colorimetrically.…”

“…This procedure was used because methanol completely destroys the vesicles, leaving free curcumin 15 . EE for curcumin was calculated as 38 :…”

Use of Curcuma longa in cosmetics: extraction of curcuminoid pigments, development of formulations, and in vitro skin permeation studies

“…In the present study, greater retention was observed, in the µg/g range; results were expressed in grams of skin because non-dermatomed pig ear skin has variable thickness (0.95 -1.45 mm in this study). In another investigation, skin retention of liposomeencapsulated curcumin was in the µg/cm 2 range in experiments with a duration of up to 50 hours (Chen et al, 2012). Parameters that affect the skin permeation of a substance and should be taken into account include the size of the molecule, its polarity, and its partition coefficient.…”

In Vitro Penetration Tests of Transethosome Gel Preparations Containing Capsaicin

“…In addition, zeta potential is a measure of the charge on the surface of a particle in a specific liquid medium [8]. Stable nanoparticle suspensions should have a zeta potential value of <−30 mV or more than +30 mV [9]. Thus, suspensions must have a higher repulsive force and a stable system to prevent the aggregation of the particle.…”