Clarithromycin-Loaded Ocular Chitosan Nanoparticle: Formulation, Optimization, Characterization, Ocular Irritation, and Antimicrobial Activity

被引:57
作者
Bin-Jumah, May [1 ]
Gilani, Sadaf Jamal [2 ]
Jahangir, Mohammed Asadullah [3 ]
Zafar, Ameeduzzafar [4 ]
Alshehri, Sultan [5 ,6 ]
Yasir, Mohd [7 ]
Kala, Chandra [8 ]
Taleuzzaman, Mohamad [8 ]
Imam, Syed Sarim [5 ]
机构
[1] Princess Nourah Bint Abdulrahman Univ, Coll Sci, Biol Dept, Riyadh, Saudi Arabia
[2] Princess Nourah Bint Abdulrahman Univ, Dept Basic Hlth Sci, Riyadh, Saudi Arabia
[3] Nibha Inst Pharmaceut Sci, Dept Pharmaceut, Nalanda 803116, Bihar, India
[4] Jouf Univ, Coll Pharm, Dept Pharmaceut, Sakaka, Aljouf, Saudi Arabia
[5] King Saud Univ, Coll Pharm, Dept Pharmaceut, Riyadh, Saudi Arabia
[6] Almaarefa Univ, Coll Pharm, Riyadh, Saudi Arabia
[7] Arsi Univ, Coll Hlth Sci, Dept Pharm, Asella, Ethiopia
[8] Maulana Azad Univ, Fac Pharm, Jodhpur 342802, Rajasthan, India
来源
INTERNATIONAL JOURNAL OF NANOMEDICINE | 2021年 / 15卷
关键词
clarithromycin; chitosan; optimization; nanoparticles; HET-CAM; antimicrobial assessment; IN-VITRO; DELIVERY; VIVO; DORZOLAMIDE; CARRIERS;
D O I
10.2147/IJN.S269004
中图分类号
TB3 [工程材料学];
学科分类号
0805 ; 080502 ;
摘要
Purpose: The topically administered drugs through conventional delivery systems have low bioavailability. Henceforth, the present study was designed to prepare and optimize clarithromycin (CTM)-loaded chitosan nanoparticles (CHNPs) to demonstrate the efficacy against microorganisms. Methods: Clarithromycin-loaded chitosan nanoparticles (CTM-CHNPs) were prepared by ionotropic gelation method. The formulation was optimized by box-Behnken design using the formulation variables like CH (A), STPP concentration (B), and stirring speed (C). Their effects were evaluated on the independent variables like particle size (Y-1) and entrapment efficiency (Y-2). Further, CTM-CHNPs were evaluated for physicochemical parameters, in-vitro drug release, ex-vivo permeation, bioadhesive study, corneal hydration, histopathology, HET-CAM, and antibacterial study. Results: The optimized formulation (CTM-CHNPopt) showed the low particle size (152 +/- 5 nm), which is desirable for ocular delivery. It also showed high encapsulation (70.05%), zeta potential (+35.2 mV), and was found in a spherical shape. The drug release study revealed a sustained drug release profile (82.98 +/- 3.5% in 12 hours) with Korsmeyer peppas kinetic (R-2=0.996) release model. It showed a 2.7-fold higher corneal permeation than CTM-solution. CHNPs did not exhibit any sign of damage to excised goat cornea, which is confirmed by hydration, histopathology, and HET-CAM test. It exhibited significant (P<0.05) higher antibacterial susceptibility than CTM-solution. Conclusion: The finding of the study concluded that CTM-CHNPs can be used for effective management of bacterial conjunctivitis by increasing the precorneal residence time.
引用
收藏
页码:7861 / 7875
页数:15
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