Comparison of PLGA and lecithin/chitosan nanoparticles for dermal targeting of betamethasone valerate

Abstract

Poly(lactide-co-glycolide) (PLGA) and lecithin/chitosan (LC) nanoparticles were prepared to evaluate the difference in the behavior upon administration on skin, for steroidal treatment. For this purpose, betamethasone-17-valerate (BMV)-loaded nanoparticles with a narrow size distribution and high entrapment efficiency were prepared. Permeation studies showed that both polymeric nanoparticles enhanced the amount of BMV in epidermis, which is the target site of topical steroidal treatment, when compared with commercial formulation. 1.58-Fold increase was determined in the epidermis concentration of BMV by LC nanoparticles with respect to PLGA nanoparticles. Nanoparticles were diluted in chitosan gel (10%, w/w) to prepare suitable formulation for topical application. Accumulation from both gel formulations were found significantly higher than commercial formulation in skin layers (p < 0.05). In addition, pharmacodynamic responses were also investigated as anti-inflammatory and skin-blanching parameters. Both formulations significantly improved these parameters although they contained 10 times less amount of BMV than commercial cream. Moreover, TEWL measurement exhibited no barrier function changes upon the application of nanoparticles on skin. Overall, both nanoparticles improved the localization of BMV within skin layers; but when compared with PLGA nanoparticles, the LC nanoparticles could be classified as a better candidate for topical delivery vehicle in the treatment of various dermatological inflammatory diseases.

Nanodrug administration routes

“…The adhesion assay results predicted the skin penetration/permeation behavior, since the CS gel containing nanocapsules led to a higher amount of capsaicinoids in the epidermis and dermis. In a similar work, PLGA nanoparticles and lecithin/CS nanoparticles containing betamethasone-17--valerate enhanced the amount of the drug in the epidermis when compared with the commercial formulation [109]. When nanoparticles were diluted in CS gel, accumulation in skin layers from both gel formulations was higher than the commercial formulation.…”

Nano intervention in topical delivery of corticosteroid for psoriasis and atopic dermatitis—a systematic review

“… (Zahid Hussain, et al; [ 109 ]) Diflucortolone valerate Ionic interaction Soybean lecithin; chitosan; isopropyl myristate (IPM); distilled water Improved drug accumulation in SC and epidermis [ 110 ] Betamethasone valerate PLGA nanoparticles-emulsion–diffusion–evaporation technique Lecithin/chitosan nanoparticles–ionic interaction PLGA; ethyl acetate; PVA; soybean lecithin; chitosan; ethanol; isopropyl myristate (IPM); distilled water Enhanced anti-inflammatory activity and drug epidermal concentration of lecithin/chitosan NP were observed. [ 111 ] Clobetasol propionate Ionic interaction Soybean lecithin; chitosan; isopropyl myristate (IPM); distilled water Biodegradable lecithin/chitosan NP in chitosan gel had higher anti-inflammatory activity compared to a sodium-deoxycholate gel and commercial cream. [ 112 ] Hydrocortisone-hydroxytyrosol Ionic interaction Pentasodium tripolyphosphate (TPP); chitosan In vivo and Ex vivo permeation studies revealed enhanced skin retention, contact time, and hydration.…”

“…1.58-Fold increment in the epidermal concentration of BMV by lecithin/CS NPs compared to PLGA NPs. Thus, lecithin/CS NPs were selected as a suitable candidate for topical drug delivery in the treatment of inflammatory dermal disorders [ 111 ].…”

Optimasi Formula Submikro Partikel Poly (Lactic-co-Glycolic Acid) Pembawa Betametason Valerat dengan Variasi Konsentrasi Poly (Vinyl Alcohol) dan Waktu Sonikasi

“…Permasalahan lain dari obat BMV adalah sifat obat golongan steroid ini yang praktis tidak larut air dan termasuk dalam biopharmaceutical classification system (BCS) tipe II (kelarutan rendah dan permeabilitas tinggi) [5,6]. Pembuatan obat ke dalam bentuk submikro partikel diyakini akan mampu meningkatkan luas permukaan sehingga meningkatkan kelarutan obat.…”