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Development and evaluation of extended release ciprofloxacin HCl ocular inserts employing natural and synthetic film forming agents

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Abstract

In this study, solvent casting technique was employed in fabricating ocular inserts using Pullulan as a natural film forming agent and Hydroxy propyl methyl cellulose as a synthetic film forming agent. Ciprofloxacin hydrochloride—an effective ocular antibiotic- was employed as a model drug in this study. Further modification of ciprofloxacin release from the ocuserts is obtained via coating the dual sides of the ocuserts by hydroxy ethyl cellulose as release controlling membrane. The prepared ocuserts were evaluated for various physiochemical parameters, and the in-vitro release pattern. Furthermore, accelerated stability test, sterility test, microbiological studies as well as eye irritancy test were appraised for a selected formula. All the developed ocular inserts showed that as the rate controlling membrane increased in percentage, the thickness and weight of sealed ocuserts increased. The drug content varied between 85.4 ± 16.5–98.2 ± 27.4% and the drug release followed zero-order pattern. The selected formula showed the highest sustainment effect indicated by the least release rate (16.3%/h) containing pullulan (2.0%) and dual coat of hydroxy ethyl cellulose (6.0%). Pullulan based ocular insert remained stable and intact at accelerated conditions for 30 days with overall degradation of the drug less than 2.5%. Non-irritant response in rabbits with primary irritation indices score 0 on Peyman Scale and excellent microbiological activity represented by a greater zone of inhibition (5.6 cm) compared to an ocuserts with no drug (0.8 cm) against Staphylococcus aureus. This study showed the suitability of dual sided coated Pullulan ocusert in attaining the desired sustainment effect with excellent stability.

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Acknowledgements

The authors are thankful to Dr. Nagwan Glal, Lecturer of Microbiology, Microbiology Department, Faculty of Pharmacy Al-Azhar University. This research did not receive any specific grant from funding agencies in the public, commercial, or not-for-profit sectors.

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  1. Department of Pharmaceutics, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, 11651, Egypt

    Hamdy M. Dawaba

  2. Department of Pharmaceutics, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, 11651, Egypt

    Aya M. Dawaba

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  1. Hamdy M. Dawaba
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Correspondence to Aya M. Dawaba.

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Dawaba, H.M., Dawaba, A.M. Development and evaluation of extended release ciprofloxacin HCl ocular inserts employing natural and synthetic film forming agents. J. Pharm. Investig. 49, 245–257 (2019). https://doi.org/10.1007/s40005-018-0400-x

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