Formulation, optimization and in vitro evaluation of polymer-coated liposomes encapsulating nebivolol hydrochloride
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Tarih
2023
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
Hypertension, also known as high blood pressure, is a serious medical condition that affects billions of people worldwide. Nebivolol hydrochloride, a & beta;1-adrenergic blocking agent, is used by the oral route in the treatment of hypertension and congestive heart failure. However, its lipophilic nature and poor aqueous solubility restricts its oral bioavailability. To overcome limitations related with conventional oral formulations of the drug, uncoated and polymer-coated liposomes were developed and evaluated. Liposomes loaded with nebivolol hydrochloride were prepared by thin-film hydration method and characterized. The influence of chitosan or pluronic (F127) coating on the liposome properties was evaluated in terms of physicochemical characteristics, stability in simulated gastrointestinal fluids, mucin interaction, in vitro drug release and cytotoxicity studies. It was observed that coating the liposomes with either chitosan or pluronic affected the size, surface charge and encapsulation efficiency of the formulations. The surface morphology studies confirmed the vesicular shape of liposomes. The results obtained indicated that both polymer-coated liposome formulations maintained their stability in simulated gastrointestinal fluids and showed significant in vitro interaction with mucin. Polymer-coated liposome formulations showed much better cumulative release of the drug than uncoated liposomes. No aggregation was observed at the end of four-week storage period and low toxicity in Caco-2 cells was measured. The results demonstrated that polymer coating of liposomes could enhance the in vitro release of nebivolol hydrochloride and interaction with mucin following oral administration and might be attractive alternative nanocarriers to traditional oral formulations.
Açıklama
Anahtar Kelimeler
Chitosan, Liposome, Mucin Interaction, Oral, Pluronic
Kaynak
International Journal of Polymeric Materials and Polymeric Biomaterials
WoS Q Değeri
Q3
Scopus Q Değeri
Q1
Cilt
Sayı
Künye
Sessevmez, M., Sinani, G., & Çevikelli, T. (2023). Formulation, optimization and in vitro evaluation of polymer-coated liposomes encapsulating nebivolol hydrochloride. International Journal of Polymeric Materials and Polymeric Biomaterials.
