Abstract
In this study, the encapsulation of curcumin (Cur) in “drug-in-cyclodextrin-in-liposomes (DCL)” by following the double-loading technique (DL) was proposed, giving rise to DCL–DL. The aim was to analyze the effect of cyclodextrin (CD) on the physicochemical, stability, and drug-release properties of liposomes. After selecting didodecyldimethylammonium bromide (DDAB) as the cationic lipid, DCL–DL was formulated by adding 2-hydroxypropyl-α/β/γ-CD (HPβCD)–Cur complexes into the aqueous phase. A competitive effect of cholesterol (Cho) for the CD cavity was found, so cholesteryl hemisuccinate (Chems) was used. The optimal composition of the DCL–DL bilayer was obtained by applying Taguchi methodology and regression analysis. Vesicles showed a lower drug encapsulation efficiency compared to conventional liposomes (CL) and CL containing HPβCD in the aqueous phase. However, the presence of HPβCD significantly increased vesicle deformability and Cur antioxidant activity over time. In addition, drug release profiles showed a sustained release after an initial burst effect, fitting to the Korsmeyer-Peppas kinetic model. Moreover, a direct correlation between the area under the curve (AUC) of dissolution profiles and flexibility of liposomes was obtained. It can be concluded that these “drug-in-cyclodextrin-in-deformable” liposomes in the presence of HPβCD may be a promising carrier for increasing the entrapment efficiency and stability of Cur without compromising the integrity of the liposome bilayer.
Highlights
Curcumin (Cur) is the main active component in rhizomes of Curcuma longa, which is an ancient Chinese spice that is extremely appreciated in traditional medicine remedies [1]
We can conclude that Cur got dissolved in the lipid vehicle during the formation of the lipid film, which can improve the assembly of the drug in the bilayer
The results of this study demonstrated that cholesteryl hemisuccinate (Chems) significantly affected the surface charge of vesicles, decreasing it as Chems concentration increased
Summary
Curcumin (Cur) is the main active component in rhizomes of Curcuma longa, which is an ancient Chinese spice that is extremely appreciated in traditional medicine remedies [1]. Cur is capable of forming hydrogen bonds with other Cur molecules and not with water, which reduces its solubility in this medium [3]. Due to this problem, Cur exhibits a low water solubility, which implies low bioavailability [2,4,5] To overcome these drawbacks, numerous strategies have been proposed, such as cyclodextrin complexation [4,6], or entrapment in liposomes [7,8], micelles [9,10], dendrimers [11], etc. Polymeric CD consists of native CD linked with one (dimeric) or more (polymeric) spacers These structures allow improved drug-binding abilities [14]. In some cases, the amount of CD that is required to dissolve the drug is high, and can trigger toxic effects [14]
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