Abstract
The present work has as its purpose the synthesis and characterization of a novel lipid material to be used in the preparation of solid lipid nanoparticles (SLNs) for the potential sustained release of progesterone in the vagina. For this reason, a material capable of ensuring the permanence of the formulation in the administration site for the time needed to guarantee the transmucosal absorption of the steroid was synthetized in order to reduce the number of administrations and to ensure an effective concentration of drug at the site of action. To this end, an ester, 2,3-dihydroxypropanoate of octadecyl (stearyl glycerine), containing two hydroxyl groups was initially synthesized. In particular, the hydroxyl group less sterically encumbered was functionalized with a thiol group, in a coupling reaction, with the amino acid L-cysteine. The obtained compound was characterized by FT-IR spectrometry and 1H-NMR. The functionalized lipid with L-cysteine was then used for the preparation of solid lipid nanoparticles that were loaded with progesterone. Finally, the release of progesterone from the lipid matrix based on newly synthesized ester, under conditions that simulate the vaginal physiological environment, was evaluated. All the obtained results suggest that the prepared nanoparticles could be used for the administration of progesterone, when its integration is essential, for example, in cases of threats of abortion or to increase fertility.
Highlights
The vagina, due to its anatomical position, the large surface area, the rich supply of blood, the relatively high permeability to many drugs, topically, is a highly effective site for the administration of drugs [1]
Several approaches have been tested in the last years to develop novel vaginal drug delivery system (DDS) able to ensure controlled release to obtain long-term therapeutic drug concentration after a single dose, combining the therapeutic needs and increasing, at the same time, the compliance of the patient
Excellent mucoadhesive properties are typical for hydrophilic polymers possessing charged groups and/or nonionic functional groups such as polyacrylate synthesis, polycarbophil, chitosan, cellulose derivatives, hyaluronic acid derivatives, and pectin that become adhesive once activated by moistening capable of forming hydrogen bonds with mucosal surfaces [7]
Summary
The vagina, due to its anatomical position, the large surface area, the rich supply of blood, the relatively high permeability to many drugs, topically, is a highly effective site for the administration of drugs [1]. Traditional commercial vaginal dosage formulations, such as creams, foams, gels, irrigations, and tablets, have the problem of residing in the vaginal cavity for a relatively short period due to the self-cleaning action of the vaginal tract and, usually, require more daily doses to guarantee the desired therapeutic effect [3, 4] In this context, several approaches have been tested in the last years to develop novel vaginal drug delivery system (DDS) able to ensure controlled release to obtain long-term therapeutic drug concentration after a single dose, combining the therapeutic needs and increasing, at the same time, the compliance of the patient. Intense research has been made to increase the adhesive properties of the polymers existing and to identify new materials in order to obtain a specific release based on mucoadhesion [8]
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