Poloxamer-based thermoresponsive ketorolac tromethamine in situ gel preparations: Design, characterisation, toxicity and transcorneal permeation studies

Fathalla, Zeinab; Vangala, Anil; Longman, Michael R.; Khaled, Khaled A.; Hussein, Amal K.; El-Garhy, Omar H.; Alany, Raid G.

doi:10.1016/j.ejpb.2017.01.008

Cited by 138 publications

(67 citation statements)

References 56 publications

(64 reference statements)

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“…4); when poloxamer 407 concentration increases there was a significant reduction in gelation temperature (*p less than 0.05). This is consistent with many works [20][21][22][23]. Park et al found a linear relationship between P407 concentration and sol-gel transition temperature over a concentration range of 10-25%; the transition temperature is linearly reduced when P407 concentration has been increased [24].…”

Section: Fig 3: Phase Change or Solution-gel Transition At Differentsupporting

confidence: 92%

Ophthalmic in-Situ Sustained Gel of Ciprofloxacin, Preparation and Evaluation Study

Al-bazzaz

Alkotaji

2018

Int J App Pharm

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Objective: This work aims to formulate and evaluate an ophthalmic in-situ gel of ciprofloxacin hydrochloride (HCl) using poloxamer 407 (P407) as a gelling agent and hydroxypropyl methylcellulose (HPMC) as a viscosity modifier. The objective of this work was to prolong the contact time as the in-situ gel will be converted into a gel upon contact with the cul-de-sac. Methods: Ciprofloxacin HCl ophthalmic in-situ gel was prepared by utilizing (P407) as a temperature-dependent polymer while hydroxypropyl methylcellulose was used as a viscosity modifier. The system was evaluated for physical appearance, pH, drug content, sterility, irritancy and stability. In addition, gelation temperature and a viscosity at different shear rates and different temperatures were studied. The compatibility of the polymer with ciprofloxacin was studied by using fourier transform infrared spectroscopy (FTIR). The in vitro release of the drug was also evaluated and supported by a preliminary in vivo test.Results: The results showed that the prepared formulas were clear, with acceptable pH and the drug contents were within the acceptable limits. FTIR results detected no incompatibility between poloxamer 407 and ciprofloxacin HCl. Notably, the viscosity of the system showed a pseudoplastic behaviour where a reduction in viscosity upon increasing the shear rate was observed. The in vitro release study confirmed the prolongation of the release of the optimized formula (F6) up to 8 h. Upon application of F6 into eyes of rabbits there was no irritancy. In addition, in vivo elimination study showed a prolonged contact for the in-situ gel in comparison with the rapid clearance of eye drop. Stability study indicated the stability of the optimized formula (F6). Conclusion: The prepared optimized formula (F6) represents a successful, safe, stable and prolonged release in-situ gel formula of ciprofloxacin.

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Section: Fig 3: Phase Change or Solution-gel Transition At Differentsupporting

confidence: 92%

Ophthalmic in-Situ Sustained Gel of Ciprofloxacin, Preparation and Evaluation Study

Al-bazzaz

Alkotaji

2018

Int J App Pharm

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“…The use of poloxamer 407 results in clear, colorless, transparent gels. Transparency is a highly desirable characteristic in ophthalmic formulations because non-transparent systems may blur the vision and they are not suitable for patients [ 140 ]. Gels containing the co-polymer demonstrated muco-mimetic properties and optical clarity, promoting a significant degree of ocular permeation and an increase in the bioavailability of the drugs [ 72 ].…”

Section: Poloxamer 407-based Mucoadhesive Formulationsmentioning

confidence: 99%

Mucosal Applications of Poloxamer 407-Based Hydrogels: An Overview

et al. 2018

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Poloxamer 407, also known by the trademark Pluronic® F127, is a water-soluble, non-ionic triblock copolymer that is made up of a hydrophobic residue of polyoxypropylene (POP) between the two hydrophilic units of polyoxyethylene (POE). Poloxamer 407-based hydrogels exhibit an interesting reversible thermal characteristic. That is, they are liquid at room temperature, but they assume a gel form when administered at body temperature, which makes them attractive candidates as pharmaceutical drug carriers. These systems have been widely investigated in the development of mucoadhesive formulations because they do not irritate the mucosal membranes. Based on these mucoadhesive properties, a simple administration into a specific compartment should maintain the required drug concentration in situ for a prolonged period of time, decreasing the necessary dosages and side effects. Their main limitations are their modest mechanical strength and, notwithstanding their bioadhesive properties, their tendency to succumb to rapid elimination in physiological media. Various technological approaches have been investigated in the attempt to modulate these properties. This review focuses on the application of poloxamer 407-based hydrogels for mucosal drug delivery with particular attention being paid to the latest published works.

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“…Fathalla Z.M.A. et al [32] studied the blend of the same two poloxamers for a controlled ocular delivery of ketorolac tromethamine (KT). The most promising gel formulations, loaded with KT, were those containing the mixtures of P407:P188 23:10 w/v% and 23:15 w/v% respectively.…”

Section: Poloxamers For Oftalmic Administrationmentioning

confidence: 99%

Poloxamer Hydrogels for Biomedical Applications

2019

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This review article focuses on thermoresponsive hydrogels consisting of poloxamers which are of high interest for biomedical application especially in drug delivery for ophthalmic, injectable, transdermal, and vaginal administration. These hydrogels remain fluid at room temperature but become more viscous gel once they are exposed to body temperature. In this way, the gelling system remains at the topical level for a long time and the drug release is controlled and prolonged. Poloxamers are synthetic triblock copolymers of poly(ethylene oxide)-b-poly(propylene oxide)-b-poly(ethylene oxide) (PEO-PPO-PEO), also commercially known as Pluronics®, Synperonics® or Lutrol®. The different poloxamers cover a range of liquids, pastes, and solids, with molecular weights and ethylene oxide–propylene oxide weight ratios varying from 1100 to 14,000 and 1:9 to 8:2, respectively. Concentrated aqueous solutions of poloxamers form thermoreversible gels. In recent years this type of gel has arouse interest for tissue engineering. Finally, the use of poloxamers as biosurfactants is evaluated since they are able to form micelles in an aqueous environment above a concentration threshold known as critical micelle concentration (CMC). This property is exploited for drug delivery and different therapeutic applications.

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Poloxamer-based thermoresponsive ketorolac tromethamine in situ gel preparations: Design, characterisation, toxicity and transcorneal permeation studies

Cited by 138 publications

References 56 publications

Ophthalmic in-Situ Sustained Gel of Ciprofloxacin, Preparation and Evaluation Study

Ophthalmic in-Situ Sustained Gel of Ciprofloxacin, Preparation and Evaluation Study

Mucosal Applications of Poloxamer 407-Based Hydrogels: An Overview

Poloxamer Hydrogels for Biomedical Applications

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