Chitosan-coated alginate (CCA) nanoparticles for augmentation of topical antihistaminic activity of diphenhydramine: in-vitro optimization, skin histopathology and pharmacodynamic studies with in vitro/in vivo correlation.

Autor: Aziz SN; Physicochemical Lab, Central Administration of Drug Control, Egyptian Drug Authority, Cairo, Egypt., Badawy AA; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt., Nessem DI; Department of Pharmaceutics, Egyptian Drug Authority, Cairo, Egypt., Abd El Malak NS; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.; School of Pharmacy, New Giza University NGU, New Giza, Egypt., Naguib MJ; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Jazyk: angličtina
Zdroj: Drug development and industrial pharmacy [Drug Dev Ind Pharm] 2023 Apr; Vol. 49 (4), pp. 316-327. Date of Electronic Publication: 2023 May 12.
DOI: 10.1080/03639045.2023.2211672
Abstrakt: Objective: The aim of the present study was to formulate chitosan-coated alginate nanoparticles containing the drug diphenhydramine hydrochloride (DHH).
Significance: Diphenhydramine hydrochloride (DHH) is the prototype of H 1 -antihistaminic drugs. It is a lipophilic drug, that easily crosses the blood-brain barrier when taken orally causing decrements in alertness and performance. Multiple applications of topical drug products are required. Thus, drug incorporation in nanocarriers would increase the skin penetration powers increasing the drug efficacy.
Methods: Chitosan-coated alginate (CCA) nanoparticles were prepared via polyelectrolyte complex technique adopting 2 3 full factorial designs. Three factors, namely, alginate concentration, drug-to-alginate ratio and CaCl 2 volume, each in two levels were studied. The prepared formulae were evaluated utilizing entrapment efficiency (EE), particle size (PS), polydispersity index (PDI), zeta potential (ZP) and in vitro release. The characterization process was then followed by optimization.
Results: At alginate conc. of 1%, drug to alginate ratio of 2:1 and CaCl 2 volume of 4 mL, NP8 was chosen as a candidate formula. Histopathological examination on shaved rat dorsal skin disclosed the safety of NP8 with no signs of necrosis or even inflammation. The enhanced topical delivery of diphenhydramine hydrochloride enclosed in the developed nanoparticles was further proved by induction of allergic reaction using intradermal histamine injection. The results revealed the superior ability of NP8 to decrease the diameter of the formed wheal in comparison to the marketed DHH product.
Conclusion: Thus, CCA nanoparticles are considered candidate nanocarriers for fortifying the topical antihistaminic activity of DHH.
Databáze: MEDLINE
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