Development of an Ocular Film Containing Ofloxacin in a Chitosan Matrix
Downloads
Background: Chitosan is a natural polymer that is widely used in pharmaceutical applications owing to its biodegradability and biocompatibility. High molecular weight chitosan, which is commonly found in the market (Sigma Aldrich), is acid soluble and thus limits its application for ocular purposes. Objective: This study aimed to improve the characteristics of high-MW chitosan ocular films by utilizing a water-soluble, low-MW chitosan modifier for the delivery of ofloxacin post-surgery. Methods: Various film formulas were prepared using high-MW chitosan as the main polymer matrix, glycerin and polyethylene glycol 400 as plasticizers, and low-MW chitosan as film modifiers. Glycerine was the best plasticizer that produced a good film appearance when added at an appropriate ratio, 8.33 times the weight of the high MW chitosan (TGc) and 6.25 times the weight of low- and high-MW chitosan blends at (1:1) ratio (MGb). The films were further developed as TGcs and MGbs were cross-linked using sodium tripolyphosphate to control the release of ofloxacin and improve its mechanical characteristics. Water absorption capability, mechanical characteristics, in vitro drug release, and antimicrobial activity were evaluated to determine the film formula. Results: The MGb formula showed the highest water absorption (approximately 230 %), while the lowest was shown by the TGcs formula (approximately 145 %). In contrast, the TGcs formula had the highest film elasticity (141.33±8.81%), and the MGb formula had the lowest (42.55±6.11%). Surprisingly, the best controlled release of ofloxacin for up to 24 h was produced by the MGbs film, which also showed the highest antimicrobial activity. MGbs also showed moderate film characteristics, which are suitable for ocular applications. Conclusion: The research concluded that The addition of water-soluble low-MW chitosan and a cross-linker agent can improve the controlled release and characteristics of chitosan-based ocular films.
Agnihotri, S. A., Mallikarjuna, N. N., and Aminabhavi, T. M. (2004) : Recent Advances on Chitosan-Based Micro- and Nanoparticles in Drug Delivery, Journal of Controlled Release, 100, 5-28.
Bader, H. dan Göritz, D. (1994) :Investigation on high amylose corn starch films. Part 2: Water vapor sorption, Starch-Stärke, Vol. 46 No.7, 249–252.
Barbosa, J., Berges, R., dan Sanz‐Nebot, V. (1998) : Retention behaviour of quinolone derivatives in high‐performance liquid chromatography: Effect of pH and evaluation of ionization constants, Journal Chromatogr A, 823, 411‐422.
Bormann, L., Tang-Liu, D., Kann, J., Nista, J., Frank, J., dan Akers, P. (1989) : Tear levels and systemic absorption of ofloksasin eyed rops in humans, Investigative Ophthalmology and Visual Science, 30, 247.
Bourtoom, T. (2008) : Plasticizer effect on the properties of biodegradable blend film from rice starch-chitosan, Songklanakarin Journal of Sciences and Technology, 30, 149-165.
Budavari, S. (Ed.) (1996) :The Merck Index12th edition, Merck, New Jersey, 68-75.
Burka, J. M., Bower, K. S., Vanroekel, R. C., Stutzman, R. D., Kuzmowych, C. P., dan Howard, R. S. (2005) : The Effect of Fourth-Generation FluoroquinolonesGatifloxacin and Moxifloxacin on Epithelial Healing Following Photorefractive Keratectomy, American Journal of Ophthalmology, 140, 83-87.
Chamarthy, S.P. dan Pinal, R. (2008) : Plasticizer concentration and the performance of a diffusion-controlled polymeric drug delivery system, Colloids and Surfaces A Physicochemical Eneneering Aspects, Vol.331 No.1-2, 25–30.
Chen, R. H., Lin, J. H., dan Yang, M. H. (1994) : Relationships Between The Chain Flexibilities of Chitosan Molecules and The Physical Properties of Their Casted Films. Carbohydrate Polymers, 24, 41-46.
Davis, Samuel P. (Ed.) (2011) :Chitosan : Manufacture, Properties and Usage, Nova Science Publishers, New York, 334-340.
Eduardo, Azevedo P., Tasia Saldanha, D. P., Marco Navarro, V. M., Aldo Medeiros, C., Marconi Ginani, F., and Fernanda Raffin, N. (2006) : Mechanical properties and release studies of chitosan films impregnated with silver sulfadiazine, Journal of Applied Polymer Science, 102, 3462–3470.
Kienzle-Sterzer, C. A., Rodrigeuz-Sanchez, D., danRha, C. K. (1982) : Mechanical Properties of Chitosan Films: Effect of Solvent Acid, Die Makromolekulare Chemie, 183(5), 1353-1359.
Kim, Se-Kwon (Ed.) (2011) :Chitin, Chitosan, Oligosaccharides and Their Derivatives; Biological Activities and Applications, CRC Press, New York, 37-47.
Kumar, Bhowmiek, and Duraivel (2012) : Ocular Inserts: A Novel Controlled Drug Delivery System, The Pharma Innovation Journal. Vol. 1 No. 12.
Lim, L. Y. dan Wan, Lucy (1995) : Heat Treatment of Chitosan Films, Drug Development And Industrial Pharmacy, 21 (7), 839-846.
Mainardes, R. M., Urban, M. C., Cinto, P. O., danChaud, M. V. (2005) : Colloidal carriers for ophthalmic drug delivery, Curr Drug Targets, 6, 363–371.
Martini, F. H., Nath, J. L., and Bartholomew, E. F. (2012) :Fundamentals of Anatomy and Physiolog, Pearson, United States, 555-567.
O'Brien, T. P., Maguire, M. G., Fink, N. E., Alfonso, E., dan McDonnell, P. (1995) : Efficacy of ofloksasin vs cefazolin and tobramycin in the therapy for bacterial keratitis: report from the Bacterial Keratitis Study Research Group, Arch Ophthalmol, 113, 1257-1265.
Quan, G., Tao, W. (2007) : Chitosan Nanoparticle As Protein Delivery Carrier—Systematic Examination Of Fabrication Conditions For Efficient Loading And Release,Colloid Surface B Biointerfaces,59, 24-34.
Ratajska, M., Strobin, G., Wiśniewska-Wrona, M., Ciechańska, D., Struszczyk, H., Boryniec, S., Biniaś, D., danBiniaś, W. (2003) : Studies on the biodegradation of Chitosan in an Aqueous Medium, Fibres and Textiles in Eastern Europe, Vol. 11, No. 3 (42), 75-79.
Rathore, K. S. and Nema, R. K. (2009) :Review on Ocular Inserts, International Journal of PharmTech Research, Vol.1 No.2, 164-169.
Ren, D., Yi, H., Wang, W., and Ma, X. (2005) : The Enzymatic Degradation and Swelling Properties of Chitosan Matrices with Different Degrees of N-Acetylation, Carbohydrate Research, 340, 2403–2410.
Rosen, S. L. (1993). Fundamental principles of polymeric materials, John Wiley & Sons, New York.
Sakore, S., Choudari, S., and Chakraborty, B. (2010) : Bi Owaiver Monograph For Immediate Release Solid Oral Dosage Forms: Ofloksasin, International Journal of Pharmacy and Pharmaceutical Sciences, 2, 156-161.
Snejdrova, E., Dittrich, M. (2012) : Pharmaceutically Used Plasticizer, Recent Advances in Plasticizer. Rijeka. InTech Europe.
Taghizadeh, S. M. and Davari, G. (2006) : Preparation, characterization and swelling behavior of N-acetylated and deacetylatedchitosans, Carbohydrate Polymers, 64, 9–15.
Wilson, A.S. (1995) :Plasticizers Principles and Practice, Cambrigde: The Institute of Materials, London.
Yao, Z., Han, B. Q., Wu, H.G., and Liu, W. S. (2005) : The Effect of Molecular Weight on The Biocompatibility of Chitosan Membrane to Keratocytes, Chinese Journal of Biomedical Engineering, 24 (4), 477-481.
Zhou, D. and Qiu, Y. (2010) : Understanding Material Properties in Pharmaceutical Product Development and Manufacturing : Powder Flow and Mechanical Properties, Journal of Validation Technology, 16.2, 65-77.
Copyright (c) 2024 JURNAL FARMASI DAN ILMU KEFARMASIAN INDONESIA

This work is licensed under a Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International License.
1. The copyright of this journal belongs to the Editorial Board and Journal Manager with the author's knowledge, while the moral right of the publication belong to the author.
2. The formal legal aspect of journal publication accessibility refers to the Creative Commons Attribution-Non-Commercial-Share Alike (CC BY-NC-SA), which implies that the publication can be used for non-commercial purposes in its original form.
3. Every publication (print/electronic) is open access for educational, research, and library purposes. In addition to the objectives mentioned above, the editorial board is not responsible for copyright infringement