TY - JOUR
T1 - In-vitro PHYSICOCHEMICAL PROPERTIES AND ANTIBACTERIAL ACTIVITY OF CIPROFLOXACIN-CARRAGEENAN INHALABLE MICROSPHERES
AU - Hariyadi, D. M.
AU - Hendradi, E.
AU - Rahmadi, M.
AU - Bontong, N. S.
AU - Pudjadi, E.
AU - Islam, N.
N1 - Funding Information:
This study demonstrated the potential of Ciprofloxacin HCl-Kappa Carrageenan microspheres using 0.55 to 1.0% w/v carrageenan polymers and 0.2% to 0.6% w/v of potassium chloride for inhaled DPI formulation. Increasing the concentration of carrageenan polymers and KCl crosslinker increased the size, yield, EE and DL. The outcomes of Ciprofloxacin-carrageenan microspheres revealed the efficient dispersibility of the DPI formulations. The developed formulations produced good physical characteristics, good stability and high activities against Staphylococcus aureus and Pseudomonas aeruginosa, which are the causative microbes for respiratory tract infections. Further study of in vivo activity is recommended to observe clinical applications of microspheres to measure the effectivity of the prepared formulations for lung delivery. ACKNOWLEDGEMENT The authors would like to thank the Directorate of Higher Education and Universitas Airlangga for all the support for this research under a grant of Penelitian Dasar by DRPM DIKTI No. 621/UN3.14/LT/2019.
Publisher Copyright:
© 2022, Rasayan Journal of Chemistry, c/o Dr. Pratima Sharma. All rights reserved.
PY - 2022/1/1
Y1 - 2022/1/1
N2 - This study's aim is to characterize aerosolization properties of ciprofloxacin loaded kappa-carrageenan microspheres for pulmonary delivery. Ciprofloxacin-carrageenan microspheres by ionotropic gelation were prepared and characterized for moisture content, yield, drug loading, efficiency, aerosolization properties, activity and stability. Characteristics showed spherical microspheres, smooth and size below 2µm, moisture content of <4%, yield of 46-58%, encapsulation efficiency of 40-94% and loadings of 25-37%. Optimum microspheres containing 1%w/v carrageenan and 0.6% w/v KCl, showed 58% yield, 38% loading 94.5% efficiency with slowest release. The fine particle fraction was 30%. The increased concentration of polymers from 0.5% to 1% and crosslinker from 0.2% to 0.6% significantly increased moisture content, yield, drug loading, efficiency, and aerosolization. Ciprofloxacin-carrageenan microspheres were found to be stable up to 30 days storage and have high activity against Staphylococcus aureus and Pseudomonas aeruginosa at a low dose. Inhaled ciprofloxacin-carrageenan microspheres may be useful against respiratory tract infection.
AB - This study's aim is to characterize aerosolization properties of ciprofloxacin loaded kappa-carrageenan microspheres for pulmonary delivery. Ciprofloxacin-carrageenan microspheres by ionotropic gelation were prepared and characterized for moisture content, yield, drug loading, efficiency, aerosolization properties, activity and stability. Characteristics showed spherical microspheres, smooth and size below 2µm, moisture content of <4%, yield of 46-58%, encapsulation efficiency of 40-94% and loadings of 25-37%. Optimum microspheres containing 1%w/v carrageenan and 0.6% w/v KCl, showed 58% yield, 38% loading 94.5% efficiency with slowest release. The fine particle fraction was 30%. The increased concentration of polymers from 0.5% to 1% and crosslinker from 0.2% to 0.6% significantly increased moisture content, yield, drug loading, efficiency, and aerosolization. Ciprofloxacin-carrageenan microspheres were found to be stable up to 30 days storage and have high activity against Staphylococcus aureus and Pseudomonas aeruginosa at a low dose. Inhaled ciprofloxacin-carrageenan microspheres may be useful against respiratory tract infection.
KW - Ciprofloxacin HCl
KW - Inhalable Microspheres
KW - Kappa Carrageenan
KW - Release
KW - Respiratory Infectious Diseases
KW - Stability
UR - http://www.scopus.com/inward/record.url?scp=85126991518&partnerID=8YFLogxK
U2 - 10.31788/RJC.2022.1516652
DO - 10.31788/RJC.2022.1516652
M3 - Article
AN - SCOPUS:85126991518
SN - 0974-1496
VL - 15
SP - 132
EP - 142
JO - Rasayan Journal of Chemistry
JF - Rasayan Journal of Chemistry
IS - 1
ER -