Chitosan-N-acetyl cysteine microspheres for ocular delivery of acyclovir: Synthesis and in vitro/in vivo evaluation

Rajawat, Gopal Singh; Shinde, Ujwala A.; Nair, Hema A.

doi:10.1016/j.jddst.2016.08.006

Cited by 31 publications

(10 citation statements)

References 106 publications

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“…The shifts in the peak for Amide II in SF NPs from 1537 cm −1 to 1524 cm −1 for SF/NAC NPs were possibly due to the presence of Amide II in NAC (Figure 2). There was a minor peak at 2330 cm −1 for SF/NAC NPs, which was attributed to the SH groups in NAC, as reported by other studies [36].…”

Section: A Analysis Of Atr-ftir Spectra For Examining Functions Group...supporting

confidence: 82%

Antioxidative NAC-Loaded Silk Nanoparticles with Opening Mucosal Tight Junctions for Nasal Drug Delivery: An In Vitro and In Vivo Study

Chung

Siah

et al. 2022

Pharmaceutics

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Using nasal routes to deliver drugs to the brain using multifunctional nanoparticles (NPs) to bypass the blood–brain barrier (BBB) might enhance the delivery efficacy. Anti-oxidative N-Acetyl-L-cysteine (NAC)-loaded silk fibroin (SF/NAC) NPs are produced, characterized and studied as a potential delivery vehicle for NAC delivered to the brain via nasal for both in vitro and in vivo studies. The NPs are not cytotoxic to RPMI 2650 cells, mucosal model cells, at a concentration of 6000 μg/mL. The anti-oxidative activities of SF/NAC NPs are demonstrated by high H2O2 scavenge capacities of the NPs and shown by mitochondrial superoxide (MitoSOX) immunostaining of human mesenchymal stem cells. Tight junctions in RPMI 2650 cells are opened after 30 min of incubation with SF/NAC NPs, which are demonstrated by measuring the decrease in trans-epithelial electrical resistance (TEER) values and discreteness in ZO-1 stains. The cellular uptake of SF/NAC NPs by RPMI 2650 cells is significantly greater than that for SF NPs and increased with increasing incubation time. In an in vivo imaging study (IVIS) using rats shows that the amount of NAC that is delivered to the brain by SF/NAC NPs increased by 1.40–2.60 times and NAC is retained longer in the nasal cavity than NAC solutions in a 2-h study.

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Section: A Analysis Of Atr-ftir Spectra For Examining Functions Group...supporting

confidence: 82%

Antioxidative NAC-Loaded Silk Nanoparticles with Opening Mucosal Tight Junctions for Nasal Drug Delivery: An In Vitro and In Vivo Study

Chung

Siah

et al. 2022

Pharmaceutics

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“…The formulations were prepared using emulsification crosslinking process, the microspheres having an active substance incorporation efficiency of 97.86 AE 2.06% for the chitosan microspheres and 76.99 AE 1.14% for the thiolate derivatives. In vitro release studies showed an initial burst followed by a sustained release of acyclovir for 12 h, and in vivo studies did not indicate signs of ocular toxicity [128].…”

Section: Microspheresmentioning

confidence: 90%

Chitosan: A Good Candidate for Sustained Release Ocular Drug Delivery Systems

Popa¹,

Ghica²,

Dinu-Pîrvu³

et al. 2018

Chitin-Chitosan - Myriad Functionalities in Science and Technology

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This chapter focuses on the eye, one of the most important organs of humans. Current data on pathophysiology of the human eye are presented in direct correlation with a range of therapeutic products, with a well-known and widely used material, namely chitosan. Applications of chitosan biopolymer are described in the development of innovative, modern, therapeutic devices and solutions. Thus, chitosan is a good excipient either for classic drop-type ocular systems, as well as for complex drug systems such as nanostructures (nanoparticles, nanomicelles and nanosuspensions), liposomes, microemulsions, microspheres, in situ hydrogels and inserts or implants. A number of disadvantages for ocular administration of the drugs are thus overcome.

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“…Rajawat et al reported a thiolated CS derivative, 6 in Scheme 1, as a microcarrier for the ocular delivery of acyclovir [195]. N-Acetylcysteine was covalently bonded to CS via a carbodiimide-mediated coupling reaction.…”

Section: Nanoparticles From Modified Chitosanmentioning

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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Chitosan-N-acetyl cysteine microspheres for ocular delivery of acyclovir: Synthesis and in vitro/in vivo evaluation

Abstract: This paper presents the main aspects regarding the production of biodegradable microspheres, the optimization of parameters in the drug encapsulation process, the techniques available for polymeric systems sterilization and the effects of γ-irradiation on microparticles.

Cited by 31 publications

References 106 publications

Antioxidative NAC-Loaded Silk Nanoparticles with Opening Mucosal Tight Junctions for Nasal Drug Delivery: An In Vitro and In Vivo Study

Antioxidative NAC-Loaded Silk Nanoparticles with Opening Mucosal Tight Junctions for Nasal Drug Delivery: An In Vitro and In Vivo Study

Chitosan: A Good Candidate for Sustained Release Ocular Drug Delivery Systems

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

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