May Bin-Jumah1, Sadaf Jamal Gilani2, Mohammed Asadullah Jahangir3, Ameeduzzafar Zafar4, Sultan Alshehri5,6, Mohd Yasir7, Chandra Kala8, Mohamad Taleuzzaman8, Syed Sarim Imam5. 1. Biology Department, College of Science, Princess Nourah Bint Abdulrahman University, Riyadh, Saudi Arabia. 2. Department of Basic Health Sciences, Princess Nourah Bint Abdulrahman University, Riyadh, Saudi Arabia. 3. Department of Pharmaceutics, Nibha Institute of Pharmaceutical Sciences, Rajgir, Nalanda 803116, Bihar, India. 4. Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Aljouf, Saudi Arabia. 5. Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia. 6. College of Pharmacy, Almaarefa University, Riyadh, Saudi Arabia. 7. Department of Pharmacy, College of Health Science, Arsi University, Asella, Ethiopia. 8. Faculty of Pharmacy, Maulana Azad University, Jodhpur 342802, Rajasthan, India.
Abstract
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 (Y1) and entrapment efficiency (Y2). 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 (R2=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.
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 (Y1) and entrapment efficiency (Y2). 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 (R2=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.
Authors: Mariana M Silva; Raquel Calado; Joana Marto; Ana Bettencourt; António J Almeida; Lídia M D Gonçalves Journal: Mar Drugs Date: 2017-12-01 Impact factor: 5.118
Authors: Mohd Abul Kalam; Muzaffar Iqbal; Abdullah Alshememry; Musaed Alkholief; Aws Alshamsan Journal: Molecules Date: 2022-04-04 Impact factor: 4.411