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Review
. 2018 Oct 9;16(10):373.
doi: 10.3390/md16100373.

Chitosan-Based In Situ Gels for Ocular Delivery of Therapeutics: A State-of-the-Art Review

Teodora Irimia  1 , Cristina-Elena Dinu-Pîrvu  2 , Mihaela Violeta Ghica  3 , Dumitru Lupuleasa  4 , Daniela-Lucia Muntean  5 , Denisa Ioana Udeanu  6 , Lăcrămioara Popa  7
Affiliations
Review

Chitosan-Based In Situ Gels for Ocular Delivery of Therapeutics: A State-of-the-Art Review

Teodora Irimia et al. Mar Drugs. .

Abstract

Ocular in situ gels are a promising alternative to overcome drawbacks of conventional eye drops because they associate the advantages of solutions such as accuracy and reproducibility of dosing, or ease of administration with prolonged contact time of ointments. Chitosan is a natural polymer suitable for use in ophthalmic formulations due to its biocompatibility, biodegradability, mucoadhesive character, antibacterial and antifungal properties, permeation enhancement and corneal wound healing effects. The combination of chitosan, pH-sensitive polymer, with other stimuli-responsive polymers leads to increased mechanical strength of formulations and an improved therapeutic effect due to prolonged ocular contact time. This review describes in situ gelling systems resulting from the association of chitosan with various stimuli-responsive polymers with emphasis on the mechanism of gel formation and application in ophthalmology. It also comprises the main techniques for evaluation of chitosan in situ gels, along with requirements of safety and ocular tolerability.

Keywords: chitosan; in situ gels; mucoadhesion; ocular delivery; sol–gel transition.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Chemical structure of chitosan.
Figure 2
Figure 2
Protonation of chitosan in acidic medium.
Figure 3
Figure 3
Chemical structure of Carbopol (Polyacrilic acid).
Figure 4
Figure 4
Chemical structure of poloxamer (Pluronic®).
Figure 5
Figure 5
Neutralization of chitosan with β-glycerophosphate.
Figure 6
Figure 6
Cross-linking of chitosan with genipin.
Figure 7
Figure 7
Poly (N-isopropylacrylamide)-chitosan interaction.
Figure 8
Figure 8
Hybrid hydrogel between chitosan and sodium alginate.
See this image and copyright information in PMC

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