Formulation and characterization of poloxamer 407®: thermoreversible gel containing polymeric microparticles and hyaluronic acid

Pereira, Gabriela Garrastazu; Dimer, Frantiescoli Anversa; Guterres, Sílvia Stanisçuaski; Kechinski, Carolina Pereira; Granada, Jonas Eichelberger; Cardozo, Nilo Sérgio Medeiros

doi:10.1590/s0100-40422013000800008

Cited by 58 publications

(40 citation statements)

References 27 publications

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“…In a previous study the phase transition temperature (Tsol-gel) and rheological properties of poloxamer 407 gel were evaluated [19]. Tsol-gel reduced (without compromising the gel strength) and pseudoplastic rheology was observed upon the addition of microparticles (or drug).…”

Section: Discussionmentioning

confidence: 99%

Preparation and assessment of ketamine hydrogels for prolonged transdermal anaesthesia

Liu¹,

Zheng²

2017

Trop. J. Pharm Res

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Section: Discussionmentioning

confidence: 99%

Preparation and assessment of ketamine hydrogels for prolonged transdermal anaesthesia

Liu¹,

Zheng²

2017

Trop. J. Pharm Res

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“…The viscosities of F11 and Rozex ® were similar. Through this data, we also determined the pseudoplastic behavior of the formulations observed; the viscosity decreases as the shear rate increases (Pereira et al, 2013;Ricci et al, 2002). It is worth adding that, in general, formulations containing P407 gels offer the advantage of thixotropic behavior.…”

Section: Sol-gel Transition Temperaturementioning

confidence: 99%

“…It is worth adding that, in general, formulations containing P407 gels offer the advantage of thixotropic behavior. This is a desirable characteristic when the intention is to facilitate the administration and spreadability in open wounds in order to avoid friction of the gel, thus reducing the suffering of the patient (Ricci et al, 2002;Pereira et al, 2013). The viscosity values apparent at 20 s -1 for the thermosensitive gels were 4.4 Pa ± 1.2 for the F12 gel, 6.5 Pa ± 1.0 for the F11 gel and 7.2 Pa ± 0.6 for Rozex ® .…”

Section: Sol-gel Transition Temperaturementioning

confidence: 99%

“…This stage precedes the gel formation of the system. Besides this, regarding Ivanova (2002), the presence of the PG decreases the lattice spacing, leading to the formation of more compact systems, culminating in the increase of the apparent viscosity of the F11 system in relation to F12 (Ivanova, Lindman, Alexandridis, 2002;Miller, Drabik, 1984;Pereira et al, 2013).…”

Section: Sol-gel Transition Temperaturementioning

confidence: 99%

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Metronidazole thermogel improves retention and decreases permeation through the skin

Melo

Araujo

Silva

et al. 2017

Braz. J. Pharm. Sci.

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Metronidazole (MTZ) is widely used as the standard antibiotic for the treatment of rosacea and, more recently, is being used off label in Brazilian hospitals for the treatment of wounds. Following oral administration, minimal amounts of active agent reaches the skin and side effects are strongly induced. Consequently, MTZ is currently being applied topically in order to improve the therapeutic efficacy with reduced side effects, with Rozex ® (RZ) (an MTZ gelled formulation) being the only marketed product. This study examined whether the use of MTZ 0.75% from thermogel formulations could improve drug retention and reduce dermal exposure compared to that by Rozex ® . Following a 21 h permeation study, the highest total amount of MTZ permeated through the rat healthy and disturbed skin was seen with Rozex ® , but similar to all formulations regardless of the skin condition. On the other hand, the amount retained in the epidermis/dermis was larger for thermogel formulations; at least 4 fold that of Rozex ® , when the stratum corneum was present as a barrier. In conclusion, thermogel formulations can be favorable alternatives to Rozex ® for the topical application of MTZ with improved efficacy and reduced side effects.Uniterms: Metronidazole/evaluation. Metronidazole/drug retention. Poloxamer 407. Rosacea/treatment. Dermatopharmacokinetic.

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“…6,7 Poloxamer solution forms a clear solution at 4-5°C and converts to gel at room temperature. 8 Rate controlling membranes were formulated by using E RLPO and E RSPO, the effect of penetration enhancer on release kinetics was evaluated.…”

Section: Introductionmentioning

confidence: 99%

Formulation Optimization and Study on Effect of Penetration Enhancers on Reservoir Transdermal Therapeutic Systems of Hydralazine Hydrochloride

Mannam¹,

Yallamalli²

2017

JYP

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INTRODUCTIONPulmonary arterial hypertension is a progressive disease which is due to constriction of pulmonary artery by excessive production of endothelien receptors. Hydralazine hydrochloride (HZH) is a drug candidate used to treat pulmonary arterial hypertension and it acts as a vasodilator by relaxing smooth muscles of pulmonary artery and the treatment lasts for long time. 1,2 Extreme variability in oral dosing of HZH, bioavailability of 31% and variable half-life of 3 to 7 h has made the dosage regimen complicated for oral usage.3 Metabolism variations depending on the phenotype and food interactions had much narrowed its oral usage. Low bioavailability, variable and short half-life may not be suitable to meet the therapeutic needs of the patient where the treatment is for longer duration. There is a need for alternative to oral route where hepatic first pass metabolism can be excluded and which can improve the therapeutic activity and quality of life of patient. As the drug has of low molecular weight 196.6 Daltons 4 transdermal delivery is a better alternative to oral route, where a continuous infusion of drug can be provided and patient compliance can be improved. Transdermal systems with a rate control membrane can provide a relatively constant rate of infusion of drug when the drug was maintained in required concentrations in reservoir system where the release rate will depend upon permeation through rate controlling membrane. 5 Hence, in the present work gel drug reservoir of HZH was formulated and the release rate was controlled by using rate controlling membrane and by varying penetration enhancers.Gel reservoir was formulated by using poloxamer a temperature sensitive hydrogel which is very stable, biocompatible and biodegradable polymer. 6,7 Poloxamer solution forms a clear solution at 4-5°C and converts to gel at room temperature.8 Rate controlling membranes were formulated by using E RLPO and E RSPO, the effect of penetration enhancer on release kinetics was evaluated. Pharmacotechnical properties, in vitro, ex vivo studies, stability studies and in vivo pharmacokinetic studies were evaluated. MATERIALS AND METHODS MaterialsHydralazine Hydrochloride was a gift sample received from Hetero drugs Pvt. Ltd, Hyderabad. Poloxamer 407 was provided as gift sample by Hi-Media Laboratories, Mumbai. Eudragit RLPO (E RLPO) and Eudragit RSPO (E RSPO) were gift samples provided by Zhaveri Pharma Chemicals., Mumbai. Release liner (poly iso butylene tape) was purchased from 3M. Hydroxy Propyl Methyl Cellulose (HPMC) and Poly Vinyl Acetate (PVA) were purchased from Hi-Media Laboratories, Mumbai. Azone (AZ), isopropyl myristate (IPM) and menthol (MT) were purchased from S.D Fine chemicals, Mumbai, India. All the solvents and reagents used were of analytical grade. Measurement of sol-gel transition temperatureSol-gel transition temperature was done to determine the poloxamer 407 concentration which retains its gel formation properties at room temperature. Poloxamer 407 solution with different concentrations ABST...

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Formulation and characterization of poloxamer 407®: thermoreversible gel containing polymeric microparticles and hyaluronic acid

Cited by 58 publications

References 27 publications

Preparation and assessment of ketamine hydrogels for prolonged transdermal anaesthesia

Preparation and assessment of ketamine hydrogels for prolonged transdermal anaesthesia

Metronidazole thermogel improves retention and decreases permeation through the skin

Formulation Optimization and Study on Effect of Penetration Enhancers on Reservoir Transdermal Therapeutic Systems of Hydralazine Hydrochloride

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