D-Optimal Design in the Development of Rheologically Improved In Situ Forming Ophthalmic Gel

Krtalić, Iva; Radošević, Senka; Hafner, Anita; Grassi, Mario; Nenadić, Mirta; Cetina-Čižmek, Biserka; Filipović-Grčić, Jelena; Pepić, Ivan; Lovrić, Jasmina

doi:10.1016/j.xphs.2018.01.019

Cited by 41 publications

(20 citation statements)

References 46 publications

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“…When in vitro release of bupivacaine hydrochloride was studied, it was observed that increasing the P407 concentration resulted in a lower diffusion coefficient and thus a slower release rate. Krtalic et al studied mixtures of two different poloxamers (P407 and P188) with CS prepared by a modified "cold method" [236]. The rheological properties versus the concentrations of the three polymers were studied, and mathematical equations were established to describe the dependence of the gelation temperature (T gel ), complex viscosity, and storage modulus on the composition of the hydrogel.…”

Section: Non-ionic Polymersmentioning

confidence: 99%

Chitosan and its Derivatives for Ocular Delivery Formulations: Recent Advances and Developments

et al. 2020

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Chitosan (CS) is a hemi-synthetic cationic linear polysaccharide produced by the deacetylation of chitin. CS is non-toxic, highly biocompatible, and biodegradable, and it has a low immunogenicity. Additionally, CS has inherent antibacterial properties and a mucoadhesive character and can disrupt epithelial tight junctions, thus acting as a permeability enhancer. As such, CS and its derivatives are well-suited for the challenging field of ocular drug delivery. In the present review article, we will discuss the properties of CS that contribute to its successful application in ocular delivery before reviewing the latest advances in the use of CS for the development of novel ophthalmic delivery systems. Colloidal nanocarriers (nanoparticles, micelles, liposomes) will be presented, followed by CS gels and lenses and ocular inserts. Finally, instances of CS coatings, aiming at conferring mucoadhesiveness to other matrixes, will be presented.

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Section: Non-ionic Polymersmentioning

confidence: 99%

Chitosan and its Derivatives for Ocular Delivery Formulations: Recent Advances and Developments

et al. 2020

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“…High values of G’ and G” were due to the presence of chitosan in the system. They revealed high mechanical strength of gels [ 8 ].…”

Section: Evaluation Of Ocular In Situ Gels Based On Chitosanmentioning

confidence: 99%

“…Chitosan is a suitable candidate in ophthalmic formulations due to its biocompatibility, biodegradability, mucoadhesive character, permeation enhancement and corneal wound healing effects, and antimicrobial and antifungal properties. It has pseudoplastic and viscoelastic characteristics that do not disturb the tear film [ 8 , 9 ].…”

Section: Introductionmentioning

confidence: 99%

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

et al. 2018

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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.

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“…3). This ratio was based on the approximate volumes of an eye-drop (40 µL) and a tear film (7 µL) (34,35). In a short time period after eye-drop instillation, positively charged oil droplets should electrostatically interact with negatively charged mucins in order to decrease their clearance from the ocular surface.…”

Section: In Vitro Mucoadhesion Determinationmentioning

confidence: 99%

In vitro evaluation of stearylamine cationic nanoemulsions for improved ocular drug delivery

et al. 2019

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Oil-in-water nanoemulsions (NEs) represent one of the formulation approaches to improve eye-related bio-availability of lipophilic drugs. The potential of cationic NEs is pronounced due to the electrostatic interaction of positively charged droplets with negatively charged mucins present in the tear film, providing prolonged formulation residence at the ocular surface. The aim of this study was to develop a cationic ophthalmic NE with cationic lipid stearylamine (SA) as a carrier of a positive charge. The addition of a nonionic surfactant provided the dual electro-steric stabilization of NEs and enabled tuning of SA concentration to achieve an optimal balance between its interaction with mucins and biocompatibility. Physicochemical characterization, stability profile, in vitro mucoadhesion study and biocompatibility study employing 3D HCE-T cell-based model of corneal epithelium pointed out the NE with 0.05 % (m/m) SA as the leading formulation. Minimizing SA content while retaining droplet/mucin interactions is of great importance for efficacy and safety of future ophthalmic drug products.

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D-Optimal Design in the Development of Rheologically Improved In Situ Forming Ophthalmic Gel

Cited by 41 publications

References 46 publications

Chitosan and its Derivatives for Ocular Delivery Formulations: Recent Advances and Developments

Chitosan and its Derivatives for Ocular Delivery Formulations: Recent Advances and Developments

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

In vitro evaluation of stearylamine cationic nanoemulsions for improved ocular drug delivery

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