In Vitro and Ex Vivo Evaluation of Nepafenac-Based Cyclodextrin Microparticles for Treatment of Eye Inflammation

Lorenzo-Veiga, Blanca; Díaz‐Rodríguez, Patricia; Alvarez‐Lorenzo, Carmen; Loftsson, Þorsteinn; Sigurđsson, Hákon Hrafn

doi:10.3390/nano10040709

Cited by 28 publications

(7 citation statements)

References 67 publications

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“…Recent research on ocular formulations containing CDs include: sustained-delivery eye drops [ 90 , 91 ]; in situ gelling systems [ 92 , 93 ]; mucoadhesive hydrogels [ 94 , 95 ]; CD/drug-loaded contact lenses [ 96 , 97 ]; and micro and nanosystems [ 86 , 98 , 99 ]. Also, CD-based formulations have shown potential to treat eye posterior segment diseases, such as diabetic retinopathy and age-related macular degeneration, which are commonly treated by intravitreal drug injections [ 100 ].…”

Section: Resultsmentioning

confidence: 99%

Technological evolution of cyclodextrins in the pharmaceutical field

Rincón-López

Almanza-Arjona

Riascos

et al. 2021

Journal of Drug Delivery Science and Technology

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We herein disclose how global cyclodextrin-based pharmaceutical technologies have evolved since the early 80s through a 1998 patents dataset retrieved from Derwent Innovation Index. We used text-mining techniques based on the patents semantic content to extract the knowledge contained therein, to analyze technologies related to the principal attributes of CDs: solubility, stability, and taste-masking enhancement. The majority of CDs pharmaceutical technologies are directed toward parenteral aqueous solutions. The development of oral and ocular formulations is rapidly growing, while technologies for nasal and pulmonary routes are emerging and seem to be promising. Formulations for topical, transdermal, vaginal, and rectal routes do not account for a high number of patents, but they may be hiding a great potential, representing opportunity research areas. Certainly, the progress in materials sciences, supramolecular chemistry, and nanotechnology, will influence the trend of that, apparently neglected, research. The bottom line, CDs pharmaceutical technologies are still increasing, and this trend is expected to continue in the coming years. Patent monitoring allows the identification of relevant technologies and trends to prioritize research, development, and investment in both, academia and industry. We expect the scope of this approach to be applied in the pharmaceutical field beyond CDs technological applications.

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Section: Resultsmentioning

confidence: 99%

Technological evolution of cyclodextrins in the pharmaceutical field

Rincón-López

Almanza-Arjona

Riascos

et al. 2021

Journal of Drug Delivery Science and Technology

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“…Cytokines and other mediators play essential roles in eye inflammation. 48 In this study, we examined the secretion of two inflammatory mediators, IL-1Beta and hs- CRP, in mice treated with MOX-LPs and MOX solution to determine their inflammation or irritation effect. It was found that mice with MRSA corneal infection, which were treated with MOX LPs and MOX solution, did not show any significant increase in the serum level of these inflammatory cytokines (IL-1Beta and hs-CRP) compared to a negative control (without treatment or infection) ( Figure 10 ).…”

Section: Resultsmentioning

confidence: 99%

Tailoring Terpesomes and Leciplex for the Effective Ocular Conveyance of Moxifloxacin Hydrochloride (Comparative Assessment): In-vitro, Ex-vivo, and In-vivo Evaluation

Albash¹,

Abdellatif²,

Hassan³

et al. 2021

IJN

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Aim To compare the ability of both terpesomes (TPs) and leciplex (LPs) loaded moxifloxacin hydrochloride (MOX) for enhancing ocular drug conveyance. Methods Two separate 2 1 .3 1 full-factorial trials were established to determine the influence of multiple variables upon nanovesicles properties and select the optimized formulae using Design Expert ® software. The thin-film hydration method was used to formulate TPs, while the single-step procedure was used for LPs. All formulae were characterized for their entrapment efficiency percent (EE%), particle size distribution (PS), polydispersity index (PDI), and zeta potential (ZP). Then, the optimized formulae were selected, evaluated, and compared for additional assessments. Results The optimized formulae TP4 and LP1 showed EE% of 84.14±0.21 and 78.47±0.17%, PS of 578.65±5.65 and 102.41±3.39 nm, PDI of 0.56±0.04 and 0.28±0.01, ZP of −12.50±0.30 and 32.50±0.50 mV, respectively. Further, LP1 showed enhanced corneal permeation across cow cornea compared to MOX solution and TP4. Besides, confocal laser scanning microscopy assessment viewed valuable infiltration from the fluoro-labeled LP through corneal layers compared to TP. LP1 showed spherical morphology and, its ability to adhere to mucus membranes was justified. Further, LP1 showed superiority over MOX solution in biofilm inhibition and eradication in addition to the treatment of infected mice with methicillin-resistant Staphylococcus aureus without any inflammatory response. Finally, the histopathological study verified the harmlessness and biocompatibility of the assembled LPs. Conclusion The gained outcomes confirmed the capability of utilizing LPs as a successful nanovesicle for the ocular conveyance of MOX over TPs and MOX solution.

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“…The corneal epithelium, esterase, is 2.5-fold more as compared to the endothelium and stroma [86]. An example is the nepafenac prodrug, used for inflammation and the pain associated with cataract surgery [87]. This shows that lipid vesicles are compatible with the corneal epithelium and leads to enhanced solubility and ease of transportation, across the cornea.…”

Section: Strategies For Enhancing Ocular Drug Delivery Systemmentioning

confidence: 99%

Cellulosic Polymers for Enhancing Drug Bioavailability in Ocular Drug Delivery Systems

et al. 2021

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One of the major impediments to drug development is low aqueous solubility and thus poor bioavailability, which leads to insufficient clinical utility. Around 70–80% of drugs in the discovery pipeline are suffering from poor aqueous solubility and poor bioavailability, which is a major challenge when one has to develop an ocular drug delivery system. The outer lipid layer, pre-corneal, dynamic, and static ocular barriers limit drug availability to the targeted ocular tissues. Biopharmaceutical Classification System (BCS) class II drugs with adequate permeability and limited or no aqueous solubility have been extensively studied for various polymer-based solubility enhancement approaches. The hydrophilic nature of cellulosic polymers and their tunable properties make them the polymers of choice in various solubility-enhancement techniques. This review focuses on various cellulose derivatives, specifically, their role, current status and novel modified cellulosic polymers for enhancing the bioavailability of BCS class II drugs in ocular drug delivery systems.

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In Vitro and Ex Vivo Evaluation of Nepafenac-Based Cyclodextrin Microparticles for Treatment of Eye Inflammation

Cited by 28 publications

References 67 publications

Technological evolution of cyclodextrins in the pharmaceutical field

Technological evolution of cyclodextrins in the pharmaceutical field

Tailoring Terpesomes and Leciplex for the Effective Ocular Conveyance of Moxifloxacin Hydrochloride (Comparative Assessment): In-vitro, Ex-vivo, and In-vivo Evaluation

Cellulosic Polymers for Enhancing Drug Bioavailability in Ocular Drug Delivery Systems

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