Development and evaluation of doxycycline niosomal thermoresponsive in situ gel for ophthalmic delivery

Gugleva, Viliana; Titeva, Stefka; Ermenlieva, Neli; Tsibranska, Sonya; Rangelov, Stanislav; Momekova, Denitsa

doi:10.1016/j.ijpharm.2020.120010

Cited by 35 publications

(17 citation statements)

References 51 publications

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“…Recently, Gugleva obtained an in situ heat-sensitive niosomal gel of antibiotic doxycycline for ophthalmic application [ 36 ]. For this purpose, in situ gel formulations based on poloxamer 407 alone and in combination with HPMC were prepared and evaluated in terms of sol-gel transition temperature, gelation time, and capacity.…”

Section: Ophthalmic Gelsmentioning

confidence: 99%

Gel-Based Materials for Ophthalmic Drug Delivery

Cassano

Gioia

Trombino

2021

Gels

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The most common route of administration of ophthalmic drugs is the topical route because it is convenient, non-invasive, and accessible to all patients. Unfortunately, drugs administered topically are not able to reach effective concentrations. Moreover, their bioavailability must be improved to decrease the frequency of administrations and their side effects, and to increase their therapeutic efficiency. For this purpose, in recent decades, particular attention has been given to the possibility of developing prolonged-release forms that are able to increase the precorneal residence time and decrease the loss of the drug due to tearing. Among these forms, gel-based materials have been studied as an ideal delivery system because they are an extremely versatile class with numerous prospective applications in ophthalmology. These materials are used in gel eye drops, in situ gelling formulations, intravitreal injections, and therapeutic contact lenses. This review is intended to describe gel-based materials and their main applications in ophthalmology.

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Section: Ophthalmic Gelsmentioning

confidence: 99%

Gel-Based Materials for Ophthalmic Drug Delivery

Cassano

Gioia

Trombino

2021

Gels

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“…The results revealed that the formed hard gel had a type III response, indicating a decrease in G′ and an increase followed by a decrease in G′′ (Hyun et al., 2002 ; Gugleva et al. 2020 ). The type III response is considered as the typical response of P407 hard gels (Li et al., 2018 ; Li & Hyun, 2018 ).…”

Section: Resultsmentioning

confidence: 99%

Poloxamer sols endowed with in-situ gelability and mucoadhesion by adding hypromellose and hyaluronan for prolonging corneal retention and drug delivery

et al. 2023

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The purpose of this study was to develop poloxamer (P407)-based in-situ thermogellable hydrogels with reducing concentration of P407 by adding hypromellose (HPMC) and with enhancing mucoadhesion of resulting hydrogels by adding hyaluronic acid (HA) for prolonging ocular delivery of hydroxypropyl-β-cyclodextrin (HPβCD)-solubilized testosterone (TES). Results demonstrated that 0.5% TES solution was successfully solubilized with adding 10% HPβCD. Non-gellable 13% P407 sol became in-situ gellable with adding 2.0-2.5% HPMC and mucoadhesibility was further imporved with adding 0.3% HA-L (low MW) or HA-H (high MW). Optimized 0.5% HPβCD-solubilized TES P407-based thermogellable hydrogels with enhancement of mucoadhesion for prolonging ocular delivery comprised 13% P407, 2.5% HPMC, and 0.3% HA-L or HA-H. Furthermore, rheological measurements under simulated eye blinking confirmed that non-thixotropic properties of optimized hydrogels could be spreaded evenly and retain a greater amount of drug-loaded hydrogels on the ocular surface for a longer period to prolong drug delivery. Compared with conventional eye drops, the prolonged residence time of optimized hydrogels from ex vivo and in vivo studies were observed, indicating relationships between rheological properties and in vivo performances. It was concluded that P407-based thermosensitive hydrogels with reducing concentration of P407 and enhancing mucoadhesion was successfully formulated by adding 2.5% HPMC and 0.3% HA in 13% P407 for potentially accomplishing effective clinical treatment of DED.

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“…According to a review of the literature, the ideal viscosity for optimal ocular administration is between 50 and 50,000 cp. The bioavailability will rise with increasing viscosity as the formulation's time spent in the cul de sac region of the eye rises [14]. As a result, viscosity values for all formulations were determined at 10 rpm at both 25 °C and 35 °C.…”

Section: Viscositymentioning

confidence: 99%

“…Ocular application of a thermosensitive in situ gel (prepared with p 407 and HPMC) loaded with ketorolac did not cause any irritation to the eye [13]. In the stability study performed with Doxycycline loaded thermosensitive in situ gels (prepared with P 408 and HPMC), it was determined that pH values, gelling temperatures and drug contents did not change at the end of the study [14].…”

Section: Introductionmentioning

confidence: 96%

Development of Besifloxacin HCL Loaded Ocular İn Situ Gels; In Vitro Characterization Study

POLAT

Ünal

2022

Ankara Ecz. Fak. Derg.

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Objective: The aim of this study is to develop in situ gel formulations containing besifloxacin hydrochloride are heat triggered, which are prepared by using different poloxomer and derivatives different polymers that will change the gelling temperature to increase corneal contact time, regulate drug release, improve ocular bioavailability and increase patient compliance increase mucoadhesion. Material and Method: Various concentrations of poloxamer 188 (P188) and poloxamer 407 (P407) were used to create the in situ forming gels. To increase the gel's capacity for bioadhesion, mucoadhesives such hydroxypropylmethyl cellulose (HPMC) or hydroxyethyl cellulose (HEC) were included in the formulations. Drug release in vitro, sol-gel transition temperature, rheological behavior, pH, clarity, and mucoadhesion force were all assessed for the produced formulations. Result and Discussion: The developed formulations' gelation temperatures ranged from 29 to 35°C. The preparations' viscosity and mucoadhesion force increased with increasing P407, HPMC, and HEC concentrations. Besifloxacin HCl forms in situ gel formulas with K1, K2, K3, and K6 suited for mucoadhesion characteristics, gelation temperature, and viscosity. These formulations exhibit pseudoplastic flow. Increasing polymer concentrations resulted in a reduction in the burst release of the formulations. However, at the end of 6 hours, drug release was finished in all formulations. The results show that in situ gels containing P407 and P188 show promise for besifloxacin HCl application

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Development and evaluation of doxycycline niosomal thermoresponsive in situ gel for ophthalmic delivery

Cited by 35 publications

References 51 publications

Gel-Based Materials for Ophthalmic Drug Delivery

Gel-Based Materials for Ophthalmic Drug Delivery

Poloxamer sols endowed with in-situ gelability and mucoadhesion by adding hypromellose and hyaluronan for prolonging corneal retention and drug delivery

Development of Besifloxacin HCL Loaded Ocular İn Situ Gels; In Vitro Characterization Study

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