Timolol-loaded ethosomes for ophthalmic delivery: Reduction of high intraocular pressure in vivo
Yükleniyor...
Tarih
2023
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Elsevier
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
The beta-adrenoceptor blocker timolol maleate (TML) is a commonly used pharmaceutical agent for the management of glaucoma. Conventional eye drops have limitations due to biological or pharmaceutical factors. Therefore, TML-loaded ethosomes have been designed to mitigate these restrictions and give a viable solution for reducing elevated intraocular pressure (IOP). The ethosomes were prepared using the thin film hydration method. Integrating the Box-Behnken experimental strategy, the optimal formulation was identified. The physicochemical characterization studies were performed on the optimal formulation. Then, in vitro release and ex vivo permeation studies were conducted. The irritation assessment was also carried out with Hen's Egg Test–Chorioallantoic Membrane model (HET-CAM), and in vivo evaluation of the IOP lowering effect was also performed on rats. The physicochemical characterization studies demonstrated that the components of the formulation were compatible with each other. The particle size, zeta potential, and encapsulation efficiency (EE%) were found as 88.23 ± 1.25 nm, -28.7 ± 2.03 mV, and 89.73 ± 0.42 %, respectively. The in vitro drug release mechanism was found as Korsmeyer-Peppas kinetics (R2=0.9923). The HET-CAM findings verified the formulation's eligibility for biological applications. The IOP measurements revealed no statistical difference (p>0.05) between the once-a-day application of the optimal formulation and the three-times-a-day application of the conventional eye drop. A similar pharmacological response was observed at lowered application frequencies. Therefore, it was concluded that the novel TML-loaded ethosomes could be a safe and efficient alternative for glaucoma treatment.
Açıklama
Anahtar Kelimeler
Box-Behnken Design, Timolol Maleate, Ethosome, HET-CAM, Ophthalmic Drug Delivery
Kaynak
International Journal of Pharmaceutics
WoS Q Değeri
Q1
Scopus Q Değeri
Q1
Cilt
640
Sayı
Künye
Üner, B., Özdemir, S., Pilevne, Ş. N., & Çelebi, A. R. C. (2023). Timolol-loaded ethosomes for ophthalmic delivery: Reduction of high intraocular pressure in vivo. International Journal of Pharmaceutics, 640, pp. 1-14. https://doi.org/10.1016/j.ijpharm.2023.123021
