N-acetylcysteine functionalized chitosan oligosaccharide-palmitic acid conjugate enhances ophthalmic delivery of flurbiprofen and its mechanisms

Sheng, Yuhui; Sun, Xingchen; Han, Jingtian; Hong, Wei; Feng, Jie; Xie, Songqiang; Li, Youjie; Yan, Fangwei; Li, Keke; Tian, Baocheng

doi:10.1016/j.carbpol.2022.119552

Cited by 11 publications

(10 citation statements)

References 43 publications

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“…RIV exhibits peaks at 1727 cm –1 and at 1409 and 1462 cm –1 , which are attributed to the carboxyl group of the ester bond and the tensile absorptions of CC bonds in the aromatic ring, respectively . The spectrum of NAC shows a peak at 2549 cm –1 , which corresponds to the S–H stretching vibration . RIV and NAC peaks are absent from C1 and C2, respectively, indicating the successful encapsulation of the APIs into the PLGA particles.…”

Section: Resultsmentioning

confidence: 99%

“…40 The spectrum of NAC shows a peak at 2549 cm −1 , which corresponds to the S−H stretching vibration. 41 RIV and NAC peaks are absent from C1 and C2, respectively, indicating the successful encapsulation of the APIs into the PLGA particles. Moreover, no new bonds or large displacements appeared on C1 and C2 spectra, indicating no chemical instability during the manufacturing process.…”

Section: ■ Materials and Methodsmentioning

confidence: 99%

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Evaluation of 3D-Printed Solid Microneedles Coated with Electrosprayed Polymeric Nanoparticles for Simultaneous Delivery of Rivastigmine and N-Acetyl Cysteine

Monou,

Andriotis,

Tzetzis

et al. 2024

ACS Appl. Bio Mater.

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In the current study, coated microneedle arrays were fabricated by means of digital light processing (DLP) printing. Three different shapes were designed, printed, and coated with PLGA particles containing two different actives. Rivastigmine (RIV) and N-acetyl-cysteine (NAC) were coformulated via electrohydrodynamic atomization (EHDA), and they were incorporated into the PLGA particles. The two actives are administered as a combined therapy for Alzheimer’s disease. The printed arrays were evaluated regarding their ability to penetrate skin and their mechanical properties. Optical microscopy and scanning electron microscopy (SEM) were employed to further characterize the microneedle structure. Confocal laser microscopy studies were conducted to construct 3D imaging of the coating and to simulate the diffusion of the particles through artificial skin samples. Permeation studies were performed to investigate the transport of the drugs across human skin ex vivo. Subsequently, a series of tape strippings were performed in an attempt to examine the deposition of the APIs on and within the skin. Light microscopy and histological studies revealed no drastic effects on the membrane integrity of the stratum corneum. Finally, the cytocompatibility of the microneedles and their precursors was evaluated by measuring cell viability (MTT assay and live/dead staining) and membrane damages followed by LDH release.

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Section: Resultsmentioning

confidence: 99%

Section: ■ Materials and Methodsmentioning

confidence: 99%

Evaluation of 3D-Printed Solid Microneedles Coated with Electrosprayed Polymeric Nanoparticles for Simultaneous Delivery of Rivastigmine and N-Acetyl Cysteine

Monou,

Andriotis,

Tzetzis

et al. 2024

ACS Appl. Bio Mater.

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“…The nanomicelles demonstrated a strong binding capacity with mucin in vitro and they increased the fluidity of the ocular membranes which was presumed to be due to the ability of the NAC thiol groups to reduce intermolecular interactions between neighboring lipid molecules. The nanomicelles successfully increased the bioavailability of flurbiprofenin, an in vivo rabbit eye model [ 158 ]. However, a practical barrier with mucoadhesive nanocarriers is that rabbit models, which are most commonly used for in vivo studies, may not bring clinically translatable results given that rabbit eyes have superior bioadhesion and higher mucus production compared to human eyes [ 159 ].…”

Section: Nano-based Dds For Anterior Segment Diseasesmentioning

confidence: 99%

Breaking Barriers in Eye Treatment: Polymeric Nano-Based Drug-Delivery System for Anterior Segment Diseases and Glaucoma

Ashkar

Jain

et al. 2023

Polymers

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The eye has anatomical structures that function as robust static and dynamic barriers, limiting the penetration, residence time, and bioavailability of medications administered topically. The development of polymeric nano-based drug-delivery systems (DDS) could be the solution to these challenges: it can pass through ocular barriers, offering higher bioavailability of administered drugs to targeted tissues that are otherwise inaccessible; it can stay in ocular tissues for longer periods of time, requiring fewer drug administrations; and it can be made up of polymers that are biodegradable and nano-sized, minimizing the undesirable effects of the administered molecules. Therefore, therapeutic innovations in polymeric nano-based DDS have been widely explored for ophthalmic drug-delivery applications. In this review, we will give a comprehensive overview of polymeric nano-based drug-delivery systems (DDS) used in the treatment of ocular diseases. We will then examine the current therapeutic challenges of various ocular diseases and analyze how different types of biopolymers can potentially enhance our therapeutic options. A literature review of the preclinical and clinical studies published between 2017 and 2022 was conducted. Thanks to the advances in polymer science, the ocular DDS has rapidly evolved, showing great promise to help clinicians better manage patients.

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“…The presence of positively charged chitosan from one side, and the thiolated polymer from the other side improved the bioavailability and adhesion ability of this nanomaterial. Encapsulation of the anti-inflammatory non-steroidal drug, flurbiprofen, inside these particles showed 2.44 fold higher permeation by adhering to the mucin layer ex vivo and 95–80% retention rate on the cell surface of monolayer and three-dimensional spheroids of human immortalized corneal epithelial cells [ 31 ]. A synthetic polymer based nanomicelle was also generated for topical ocular delivery.…”

Section: Topical Nano-formulations For Ocular Drug Deliverymentioning

confidence: 99%

Application of Convergent Science and Technology toward Ocular Disease Treatment

et al. 2023

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Eyes are one of the main critical organs of the body that provide our brain with the most information about the surrounding environment. Disturbance in the activity of this informational organ, resulting from different ocular diseases, could affect the quality of life, so finding appropriate methods for treating ocular disease has attracted lots of attention. This is especially due to the ineffectiveness of the conventional therapeutic method to deliver drugs into the interior parts of the eye, and the also presence of barriers such as tear film, blood-ocular, and blood-retina barriers. Recently, some novel techniques, such as different types of contact lenses, micro and nanoneedles and in situ gels, have been introduced which can overcome the previously mentioned barriers. These novel techniques could enhance the bioavailability of therapeutic components inside the eyes, deliver them to the posterior side of the eyes, release them in a controlled manner, and reduce the side effects of previous methods (such as eye drops). Accordingly, this review paper aims to summarize some of the evidence on the effectiveness of these new techniques for treating ocular disease, their preclinical and clinical progression, current limitations, and future perspectives.

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N-acetylcysteine functionalized chitosan oligosaccharide-palmitic acid conjugate enhances ophthalmic delivery of flurbiprofen and its mechanisms

Cited by 11 publications

References 43 publications

Evaluation of 3D-Printed Solid Microneedles Coated with Electrosprayed Polymeric Nanoparticles for Simultaneous Delivery of Rivastigmine and N-Acetyl Cysteine

Evaluation of 3D-Printed Solid Microneedles Coated with Electrosprayed Polymeric Nanoparticles for Simultaneous Delivery of Rivastigmine and N-Acetyl Cysteine

Breaking Barriers in Eye Treatment: Polymeric Nano-Based Drug-Delivery System for Anterior Segment Diseases and Glaucoma

Application of Convergent Science and Technology toward Ocular Disease Treatment

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