Mucoadhesive Chitosan Delivery System with Chelidonii Herba Lyophilized Extract as a Promising Strategy for Vaginitis Treatment

Abstract

Chelidonium majus (also known as celandine) contains pharmacologically active compounds such as isoquinoline alkaloids (e.g., chelidonine, sanguinarine), flavonoids, saponins, carotenoids, and organic acids. Due to the presence of isoquinoline alkaloids, Chelidonii herba extracts are widely used as an antibacterial, antifungal, antiviral (including HSV-1 and HIV-1), and anti-inflammatory agent in the treatment of various diseases, while chitosan is a biocompatible and biodegradable carrier with valuable properties for mucoadhesive formulations preparation. Our work aimed to prepare mucoadhesive vaginal drug delivery systems composed of Chelidonii herba lyophilized extract and chitosan as an effective way to treat vaginitis. The pharmacological safety of usage of isoquinoline alkaloids, based on MTT test, were evaluated for the maximum doses 36.34 ± 0.29 µg/mL and 0.89 ± 1.16 µg/mL for chelidonine and sanguinarine, respectively. Dissolution rate profiles and permeability through artificial membranes for chelidonine and sanguinarine after their introduction into the chitosan system were studied. The low permeability for used save doses of isoquinoline alkaloids and results of microbiological studies allow confirmation that system Chelidonii herba lyophilized extract chitosan 80/500 1:1 (w/w) is a promising strategy for vaginal use. Ex vivo studies of mucoadhesive properties and evaluation of tableting features demonstrated that the formulation containing Chelidonii herba lyophilized extract (120.0 mg) with chitosan (80/500—100.0 mg) and polymer content (HPMC—100.0 mg, microcrystalline cellulose—50.0 mg, lactose monohydrate—30.0 mg and magnesium stearate—4.0 mg) is a vaginal dosage form with prolonging dissolution profile and high mucoadhesion properties (up to 4 h).

Chitosan as Valuable Excipient for Oral and Topical Carvedilol Delivery Systems

“…The resulting layer hinders the escape of CVD particles deposited on the polymer surface, thus limiting the release rate [ 45 ]. The resulting layer decreases water entry into the core of the system and, accordingly, may promote a decrease in bioactive dissolution rate [ 45 , 46 ].…”

Development and Evaluation of Thermosensitive Hydrogels with Binary Mixture of Scutellariae baicalensis radix Extract and Chitosan for Periodontal Diseases Treatment

“…The permeability of active compounds from binary mixtures was investigated using the PAMPA GIT model according to the method described by Paczkowska et al [ 118 ]. The standards, S. baicalensis radix extract, and binary mixtures were dissolved in the donor solution adjusted to pH 6.6.…”

Prevalence and Risk Factors of Vaginal infection among women in Reproductive age group at Hassan Shami Camp

“…It is difficult to determine the actual occurrence of vaginal infections. The doctors use the word vaginitis as a synonym for infections, believing that all vulvovaginal irritations or itching, especially when accompanied by irregular secretions, are caused by microorganisms (9) .The environment of the vagina is profoundly affected by the level of the hormone oestradiol (10,11) . Several sociodemographic factors have been associated with reproductive tract infections, such as parity, poor socio-economic conditions, poor menstrual hygiene, and illiteracy, the diagnosis without laboratory confirmation can lead to inappropriate medication (12) Bacterial vaginosis is the most common cause of vaginal discharge among females of reproductive age.…”