Viswanadhan Vasantha Prasanth, Sherafudeen Sheri Peedikayil, Rahamathulla Mohamed, Mathew Sam Thomarayil, Murali Sandhya, Alshehri Sultan, Shakeel Faiyaz, Alam Prawez, Sirhan Ala Yahya, Narayana Iyer Bhageerathy Anantha
Department of Pharmaceutics, Mount Zion College of Pharmaceutical Sciences and Research, Chayalode P.O. Ezhamkulam, Pathanamthitta Dist, Adoor 691556, India.
Department of Pharmaceutics, Mar Discorous College of Pharmacy, Alathara, Sreekariyam, Thiruvananthapuram Dist, Thiruvananthapuram 695017, India.
Polymers (Basel). 2023 Feb 27;15(5):1206. doi: 10.3390/polym15051206.
The purpose of the study is to develop and assess mucoadhesive in situ nasal gel formulations of loratadine and chlorpheniramine maleate to advance the bioavailability of the drug as compared to its conventional dosage forms. The influence of various permeation enhancers, such as EDTA (0.2% /), sodium taurocholate (0.5% /), oleic acid (5% /), and Pluronic F 127 (10% /), on the nasal absorption of loratadine and chlorpheniramine from in situ nasal gels containing different polymeric combinations, such as hydroxypropyl methylcellulose, Carbopol 934, sodium carboxymethylcellulose, and chitosan, is studied. Among these permeation enhancers, sodium taurocholate, Pluronic F127 and oleic acid produced a noticeable increase in the loratadine in situ nasal gel flux compared with in situ nasal gels without permeation enhancer. However, EDTA increased the flux slightly, and in most cases, the increase was insignificant. However, in the case of chlorpheniramine maleate in situ nasal gels, the permeation enhancer oleic acid only showed a noticeable increase in flux. Sodium taurocholate and oleic acid seems to be a better and efficient enhancer, enhancing the flux > 5-fold compared with in situ nasal gels without permeation enhancer in loratadine in situ nasal gels. Pluronic F127 also showed a better permeation, increasing the effect by >2-fold in loratadine in situ nasal gels. In chlorpheniramine maleate in situ nasal gels with EDTA, sodium taurocholate and Pluronic F127 were equally effective, enhancing chlorpheniramine maleate permeation. Oleic acid has a better effect as permeation enhancer in chlorpheniramine maleate in situ nasal gels and showed a maximum permeation enhancement of >2-fold.
本研究的目的是开发并评估氯雷他定和马来酸氯苯那敏的黏膜黏附性原位鼻腔凝胶制剂,以提高药物相对于其传统剂型的生物利用度。研究了各种渗透促进剂,如乙二胺四乙酸(0.2% /)、牛磺胆酸钠(0.5% /)、油酸(5% /)和泊洛沙姆F 127(10% /),对含有不同聚合物组合(如羟丙基甲基纤维素、卡波姆934、羧甲基纤维素钠和壳聚糖)的原位鼻腔凝胶中氯雷他定和马来酸氯苯那敏鼻腔吸收的影响。在这些渗透促进剂中,与不含渗透促进剂的原位鼻腔凝胶相比,牛磺胆酸钠、泊洛沙姆F127和油酸使氯雷他定原位鼻腔凝胶通量显著增加。然而,乙二胺四乙酸使通量略有增加,且在大多数情况下,增加不显著。然而,对于马来酸氯苯那敏原位鼻腔凝胶,渗透促进剂油酸仅使通量显著增加。牛磺胆酸钠和油酸似乎是更好且有效的促进剂,与不含渗透促进剂的氯雷他定原位鼻腔凝胶相比,使通量提高了5倍以上。泊洛沙姆F127在氯雷他定原位鼻腔凝胶中也显示出较好的渗透性,使效果提高了2倍以上。在含有乙二胺四乙酸的马来酸氯苯那敏原位鼻腔凝胶中,牛磺胆酸钠和泊洛沙姆F127同样有效,可促进马来酸氯苯那敏的渗透。油酸作为马来酸氯苯那敏原位鼻腔凝胶中的渗透促进剂效果更好,最大渗透增强超过2倍。