• Wanachat Chaiyasan
  • Sangly P. Srinivas
  • Waree Tiyaboonchai School of Optometry, Indiana University, Bloomington, Indiana, United States


Objective: To develop and characterize a topical ophthalmic formulation containing chitosan-dextran sulfate nano particles (CDNs) for enhanced ocular bioavailability and stability of lutein.

Methods: Lutein-loaded CDNs (LCDNs) were prepared by polyelectrolyte complexation employing oppositely charged polymers, chitosan and dextran sulfate. Effects of the polymer mass ratios, the total amount of polymers, and the amount of EDC and PEG400 on their physicochemical properties as well as the drug release profiles were investigated. The physicochemical stability of LCDNs dispersed in various ophthalmic vehicles and the accompanying microbial contamination were also evaluated.

Results: LCDNs possessed a mean size of ~400 nm with a positive surface charge of+30 mV and entrapment efficiency up to 75%. Dissolution profiles followed a Higuchi's square root model, indicating a diffusional release mechanism. LCDNs dispersed in Feldman ophthalmic buffer showed good physical stability with no microbial contamination. The chemical stability of lutein was significantly improved in LCDNs and further improved by the addition of antioxidant in the ophthalmic vehicle.

Conclusion: The ophthalmic formulation containing LCDNs, developed in this work, has characteristics suitable for application in ocular surface drug delivery systems.

Keywords: Chitosan, dextran sulfate, Nanoparticles, Ophthalmic vehicle, Lutein.


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Cejka C, Cejkova J. Oxidative stress to the cornea, Changes in corneal optical properties, and advances in the treatment of corneal oxidative injuries. Oxidative Medicine Cellular Longevity 2015:10. [Article in Press]

Koushan K, Rusovici R, Li W, Ferguson LR, Chalam KV. The role of lutein in eye-related disease. Nutrients 2013;5:1823-39.

Chitchumroonchokchai C, Schwartz SJ, Failla ML. Assessment of lutein bioavailability from meals and a supplement using simulated digestion and caco-2 human intestinal cells. J Nutr 2004;134:2280-6.

Liu C-H, Chiu H-C, Wu W-C, Sahoo SL, Hsu C-Y. Novel lutein loaded lipid nanoparticles on porcine corneal distribution. J Ophthalmol 2014:11. [Article in Press]

Shi XM, Chen F. Stability of lutein under various storage conditions. Food/Nahrung 1997;41:38-41.

Kaur IP, Kanwar M. Ocular preparations: the formulation approach. Drug Dev Ind Pharm 2002;28:473-93.

Cavalli R, Gasco MR, Chetoni P, Burgalassi S, Saettone MF. Solid lipid nanoparticles (SLN) as an ocular delivery system for tobramycin. Int J Pharm 2002;238:241-5.

Chaiyasan W, Srinivas SP, Tiyaboonchai W. Mucoadhesive chitosan-dextran sulfate nanoparticles for sustained drug delivery to the ocular surface. J Ocul Pharmacol Ther 2013;29:200-7.

De Campos A, Diebold Y, Carvalho E, Sánchez A, José Alonso M. Chitosan nanoparticles as new ocular drug delivery systems: In vitro stability, in vivo fate, and cellular toxicity. Pharm Res 2004;21:803-10.

Ibrahim MM, Abd-Elgawad A-EH, Soliman OA-E, Jablonski MM. Natural bioadhesive biodegradable nanoparticles based topical ophthalmic formulations for sustained celecoxib release: in vitro study. J Pharm Technol Drug Res 2013;2:7.

Sarmento B, Ribeiro A, Veiga F, Ferreira D. Development and characterization of new insulin containing polysaccharide nanoparticles. Colloids Surf B 2006;53:193-202.

Koppel DE. Analysis of macromolecular polydispersity in intensity correlation spectroscopy: The method of cumulants. J Chem Physics 1972;57:4814-20.

McNeil-Watson F, Tscharnuter W, Miller J. A new instrument for the measurement of very small electrophoretic mobilities using phase analysis light scattering (PALS). Colloids Surf A 1998;140:53-7.

Sharma A, Dhanashree B. Screening of currency in circulation for bacterial contamination. Curr Sci India 2011;100:822-5.

Gonzalez-Mira E, Egea MA, Garcia ML, Souto EB. Design and ocular tolerance of flurbiprofen-loaded ultrasound-engineered NLC. Colloids Surf B 2010;81:412-21.

Zimmer A, Kreuter J. Microspheres, and nanoparticles used in ocular delivery systems. Adv Drug Delivery Rev 1995;16:61-73.

Tseng CL, Chen KH, Su WY, Lee YH, Wu CC, Lin FH. Cationic gelatin nanoparticles for drug delivery to the ocular surface: in vitro and in vivo evaluation. J Nanomater 2013:11. [Article in Press]

Banegas RS, Zornio CF, Borges AdMG, Porto LC, Soldi V. Preparation, characterization and properties of films obtained from cross-linked guar gum. Polímeros 2013;23:182-8.

José LA. Key aspects in nanotechnology and drug delivery. Nanotechnology and Drug Delivery, Vol. 1. CRC Press; 2014. p. 1-27.

Makadia HK, Siegel SJ. Poly lactic-co-glycolic acid (PLGA) as biodegradable controlled drug delivery carrier. Polymers 2011;3:1377-97.

Reza MS, Quadir MA, Haider SS. Comparative evaluation of plastic, hydrophobic and hydrophilic polymers as matrices for controlled-release drug delivery. J Pharm Pharm Sci 2003;6:282-91.

Bin Choy Y, Park JH, Prausnitz MR. Mucoadhesive microparticles engineered for ophthalmic drug delivery. J Phys Chem Solids 2008;69:1533-6.

Daya S, Walker RB, Glass BD, Anoopkumar-Dukie S. The effect of variations in pH and temperature on the stability of melatonin in aqueous solution. J Pineal Res 2001;31:155-8.

Khangtragool A, Ausayakhun S, Leesawat P, Laokul C, Molloy R. Chitosan as an ocular drug delivery vehicle for vancomycin. J Appl Polym Sci 2011;122:3160-7.

Fang C, Bhattarai N, Sun C, Zhang M. Functionalized nanoparticles with long-term stability in biological media. Small (Weinheim an der Bergstrasse, Germany) 2009;5:1637-41.

Liu Y, Tourbin M, Lachaize S, Guiraud P. Silica nanoparticle separation from water by aggregation with AlCl3. Ind Eng Chem Res 2012;51:1853-63.

Nair B, Elmore AR. Final report on the safety assessment of sodium sulfite, potassium sulfite, ammonium sulfite, sodium bisulfite, ammonium bisulfite, sodium metabisulfite and potassium metabisulfite. Int J Toxicol 2003;22 Suppl 2:63-88.

Mohanty B, Mishra SK, Majumdar DK. Effect of formulation factors on in vitro trans corneal permeation of voriconazole from aqueous drops. J Adv Pharm Technol Res 2013;4:210-6



How to Cite

Chaiyasan, W., S. P. Srinivas, and W. Tiyaboonchai. “DEVELOPMENT AND CHARACTERIZATION OF TOPICAL OPHTHALMIC FORMULATIONS CONTAINING LUTEIN-LOADED MUCOADHESIVE NANOPARTICLES”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 8, no. 3, Mar. 2016, pp. 261-6,



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