Microfibrillar polymeric ocular inserts for triamcinolone acetonide delivery

Prima, Giulia Di; Licciardi, Mariano; Pavia, Francesco Carfì; Monte, Attilio Ignazio Lo; Cavallaro, Gennara; Giammona, Gaetano

doi:10.1016/j.ijpharm.2019.118459

Cited by 23 publications

(17 citation statements)

References 38 publications

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“…However, it is necessary to first evaluate the aptitude of RSV to cross the selected epithelial tissue by itself, as penetration and subsequent permeation phenomena are indispensable to ensure systemic effects. The main strategy to assess the permeability of an active ingredient through a biological membrane/tissue involves the use of a two-compartment open model (e.g., Franz-type diffusion cells) accompanied by a membrane that could be synthetic and accurately designed to simulate the biological tissue or could be a biological specimen [ 34 , 37 , 38 , 39 ]. Moreover, when evaluating the permeability of poorly water-soluble molecules, it is crucial to ameliorate their solubility into the donor compartment to increase the concentration gradient, which is indispensable in establishing the permeation phenomenon.…”

Section: Resultsmentioning

confidence: 99%

Improvement of Resveratrol Permeation through Sublingual Mucosa: Chemical Permeation Enhancers versus Spray Drying Technique to Obtain Fast-Disintegrating Sublingual Mini-Tablets

et al. 2021

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Resveratrol (RSV) is a natural polyphenol with several interesting broad-spectrum pharmacological properties. However, it is characterized by poor oral bioavailability, extensive first-pass effect metabolism and low stability. Indeed, RSV could benefit from the advantage of the sublingual route of administration. In this view, RSV attitudes to crossing the porcine sublingual mucosa were evaluated and promoted both by six different chemical permeation enhancers (CPEs) as well as by preparing four innovative fast-disintegrating sublingual mini-tablets by spray drying followed by direct compression. Since RSV by itself exhibits a low permeation aptitude, this could be significantly enhanced by the use of CPEs as well as by embedding RSV in a spray-dried powder to be compressed in order to prepare fast-disintegrating mini-tablets. The most promising observed CPEs (menthol, lysine and urea) were then inserted into the most promising spray-dried excipients’ compositions (RSV-B and RSV-C), thus preparing CPE-loaded mini-tablets. However, this procedure leads to unsatisfactory results which preclude the possibility of merging the two proposed approaches. Finally, the best spray-dried composition (RSV-B) was further evaluated by SEM, FTIR, XRD and disintegration as well as dissolution behavior to prove its effectiveness as a sublingual fast-disintegrating formulation.

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Section: Resultsmentioning

confidence: 99%

Improvement of Resveratrol Permeation through Sublingual Mucosa: Chemical Permeation Enhancers versus Spray Drying Technique to Obtain Fast-Disintegrating Sublingual Mini-Tablets

et al. 2021

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“…The morphological results showed a flexible non-porous scaffold with fibers ranging from 1 to 3 μm in diameter. The surface modification allowed stable, non-erodible, mucoadhesive, and highly loaded inserts that were compatible with human cells; it also allowed extended drug release for up to 30 days [ 34 ]. Nanofiber inserts loaded with azithromycin were prepared using a mixture of chitosan, polyvinyl alcohol, and polyvinyl pyrrolidone via electrospinning.…”

Section: Resultsmentioning

confidence: 99%

“…Their large surface area enables ease of surface engineering and modification using different materials, such as permeation enhancers and mucoadhesive agents, and with the proper polymer selection, systems with controlled, sustained, and targeted release can be produced [ 31 , 32 , 33 ]. Furthermore, the produced fibers are homogeneous and highly reproducible [ 34 ], and due to their characteristic size and texture, they also represent good candidates for tissue reconstitution and promotion of human astrocytoma cell growth [ 35 ] and cell migration and proliferation [ 36 ]. A wide range of polymers are used for the fabrication of nanofibers for ocular uses, they are classified as natural, semisynthetic, and synthetic [ 37 ].…”

Section: Introductionmentioning

confidence: 99%

“…Some of the suitable polymers for the electro-spinning technique include polyesters (e.g., poly-glycolic acid- (PGA), poly-lactic acid- (PLA), polycaprolactone- (PCL)) [ 33 ]. These polymers are characterized by possessing sufficient mechanical strength to be electrospun, biocompatible, and useful for cell adhesion [ 34 ]. In some cases, a blend of the polymers is used together to control the drug release.…”

Section: Introductionmentioning

confidence: 99%

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A Systematic Review of Drug-Loaded Electrospun Nanofiber-Based Ophthalmic Inserts

Omer

Zelkó

2021

Pharmaceutics

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Currently, ocular inserts and nanoparticles have received much attention due to the limited bioavailability of conventional eye preparations and the toxicity problems of systemic drug administration. The current systematic review aims to present recent studies on the use of electrospun nanofiber-based ocular inserts to improve the bioavailability of drugs used for different ophthalmic diseases. A systematic search was performed in PubMed, Ovid Medline, Web of Science, ScienceDirect, Scopus, Reaxys, Google Scholar, and Google Patents/Espacenet taking “drug-loaded”, “nanofibers”, and “ophthalmic inserts” and their equivalent terms as keywords. The search was limited to original and peer-reviewed studies published in 2011–2021 in English language. Only 13 out of 795 articles and 15 out of 197 patents were included. All results revealed the success of nanofiber-based ocular inserts in targeting and improved bioavailability. Ocular inserts based on nanofibers can be used as safe, efficient carriers for the treatment of anterior and posterior eye diseases.

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“…1 However, with diseases such as ulcerative keratitis and acute conjunctivitis, higher therapeutic drug levels are required, as regular dose intervals of eye drops (four times per day) cannot meet the requirements owing to poor retention on the drug on the ocular surface because of tear turnover, and the innate protective mechanisms of the eye. [2][3][4] Therefore, fortified drops 5 and subconjunctival and intracameral injections are chosen in severe cases. Administration of drops every 15 min is clinically impractical and hourly administration can decrease patient compliance and increase health-care expenses.…”

Section: Introductionmentioning

confidence: 99%

<p>Comparative Assessment of Distribution Characteristics and Ocular Pharmacokinetics of Norvancomycin Between Continuous Topical Ocular Instillation and Hourly Administration of Eye Drop</p>

Lin

Zhao

Huang

et al. 2020

DDDT

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Background: The aim of this study was to compare the distribution characteristics and ocular pharmacokinetics of norvancomycin (NVCM) in ocular tissues of the anterior segment between continuous topical ocular instillation and hourly administration of eye drop in rabbits. Methods: Sixty rabbits were randomly divided into two groups: continuous topical ocular instillation drug delivery (CTOIDD) group and eye drop (control) group. In the CTOIDD group, NVCM solution (50 mg/mL) was perfused to the ocular surface using the CTOIDD system at 2 mL/ h up to 10 h and the same solution was administered at one drop (50 μL) per hour for 10 h in the control group. Animals (N=6 per time-point per group) were humanely killed at 2, 4, 6, 10, and 24 h to analyze their ocular tissues and plasma. The concentrations of NVCM in the conjunctiva, cornea, aqueous humour, iris, ciliary body and plasma were measured by HPLC with photodiode array detector. The pharmacokinetic parameters were calculated by Kinetica 5.1. Results: The highest concentrations of NVCM for the CTOIDD group and control group were 2105.45±919.89 μg/g and 97.18±43.14 μg/g in cornea, 3033.92±1061.95 μg/g and 806.99 ±563.02 μg/g in conjunctiva, 1570.19±402.87 μg/g and 46.93±23.46 μg/g in iris, 181.94 ±47.11 μg/g and 15.38±4.00 μg/g in ciliary body, 29.78±4.90 μg/mL and 3.20±1.48 μg/mL in aqueous humour, and 26.89±5.57 μg/mL and 1.90±1.87 μg/mL in plasma, respectively. The mean NVCM levels significantly increased at all time-points in cornea, iris, and ciliary body (p<0.05) in the CTOIDD group. The AUC 0-24 values in the CTOIDD group were 27,543.70 μg•h/g in cornea, 32,514.48 μg•h/g in conjunctiva, 8631.05 μg•h/g in iris, 2194.36 μg•h/g in ciliary body and 343.9 μg•h/mL in aqueous humour, which were higher than for the eye drop group in all tissues. Conclusion: Since continuous instillation of NVCM with CTOIDD could reach significantly higher concentrations and was sustained for a longer period compared with hourly administration of eye drop, CTOIDD administered NVCM could be a possible method to treat bacterial keratitis.

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Microfibrillar polymeric ocular inserts for triamcinolone acetonide delivery

Cited by 23 publications

References 38 publications

Improvement of Resveratrol Permeation through Sublingual Mucosa: Chemical Permeation Enhancers versus Spray Drying Technique to Obtain Fast-Disintegrating Sublingual Mini-Tablets

Improvement of Resveratrol Permeation through Sublingual Mucosa: Chemical Permeation Enhancers versus Spray Drying Technique to Obtain Fast-Disintegrating Sublingual Mini-Tablets

A Systematic Review of Drug-Loaded Electrospun Nanofiber-Based Ophthalmic Inserts

<p>Comparative Assessment of Distribution Characteristics and Ocular Pharmacokinetics of Norvancomycin Between Continuous Topical Ocular Instillation and Hourly Administration of Eye Drop</p>

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