Poloxamer 407/188 binary thermosensitive hydrogels as delivery systems for infiltrative local anesthesia: Physico-chemical characterization and pharmacological evaluation

Akkari, Alessandra Cristina Santos; Papini, Juliana Zampoli Boava; Garcia, Gabriella K.; Franco, Margareth K. K. D.; Cavalcanti, Leide P.; Malfatti-Gasperini, Antonio A.; Alkschbirs, Melissa I.; Yokaichyia, Fabiano; Paula, Eneida de; Tófoli, Giovana Radomille; Araújo, Daniele Ribeiro de

doi:10.1016/j.msec.2016.05.088

Cited by 94 publications

(88 citation statements)

References 41 publications

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“…Akkari and coworkers demonstrated a binary poloxamer 407/188 gel formulation as a delivery system for infiltrative local anesthesia for applications in the treatment of post-operative pain using ropivaciane as a model drug. They showed that the application of a poloxamer based formulation reduced in-vitro cytotoxic effect and increased the duration of analgesia without inducing in-vivo inflammation signs after local injection [13] . Poloxamer 407 was also used as a solubilizing agent for the formulation development of tolfenamic acid.…”

Section: Introductionmentioning

confidence: 99%

Thermogelling properties of purified poloxamer 407

Fakhari¹,

Corcoran²,

Schwarz³

2017

Heliyon

193

132

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Poloxamers are triblock copolymers with a center block of hydrophobic polypropylene oxide (PPO) flanked by two hydrophilic polyethyleneoxide (PEO) blocks. Among this family of copolymers, poloxamer 407 is a non-ionic surfactant with reversible gelation properties above a particular polymer concentration and a particular temperature. Easy preparation of poloxamer 407 based sterile injectable formulations have made this copolymer a good candidate for drug delivery, specifically when controlled release of the drug is required. Previously, the applications of compendial poloxamer 407 preparations were demonstrated; however, low viscosity, poor elasticity, and sol-to-gel transition temperature (Tsol-gel) over a wide temperature range were observed. A purification process was introduced to eliminate impurities and low molecular weight copolymer molecules from the compendial poloxamer 407 resulting in higher viscosity values with Tsol-gel in a narrow temperature range. Here, poloxamer 407 was purified based on the proposed process and the rheological and analytical evaluation of the purified poloxamer 407 was conducted and compared to unpurified, compendial poloxamer 407. Then, the impact of poloxamer 407 concentration on gel formation was evaluated. For drug delivery applications, the effect of relevant buffer salts and the effect of addition of ethanol to the poloxamer 407 solutions were rheologically evaluated.

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Section: Introductionmentioning

confidence: 99%

Thermogelling properties of purified poloxamer 407

Fakhari¹,

Corcoran²,

Schwarz³

2017

Heliyon

193

132

View full text Add to dashboard Cite

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“…They are nontoxic and biodegradable, and with proper formulation, they can increase the solubility, stability, and bioavailability of the incorporated drugs. 13 In general, HP hydrogel has been widely used for loading and delivering molecules to treat different diseases. 13,14 Recently, Wu et al developed and characterized an HP hydrogel containing acidic fibroblast growth factor (aFGF) for wound treatments and showed a clear therapeutic effect.…”

Section: Introductionmentioning

confidence: 99%

“…13 In general, HP hydrogel has been widely used for loading and delivering molecules to treat different diseases. 13,14 Recently, Wu et al developed and characterized an HP hydrogel containing acidic fibroblast growth factor (aFGF) for wound treatments and showed a clear therapeutic effect. 15 In addition, HP hydrogel loading nerve growth factor (NGF) enhanced the neuron regeneration in spinal cord injury.…”

Section: Introductionmentioning

confidence: 99%

Three-dimensional structure micelles of heparin-poloxamer improve the therapeutic effect of 17β-estradiol on endometrial regeneration for intrauterine adhesions in a rat model

Zhang¹,

Xia²,

Xu³

et al. 2017

IJN

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Intrauterine adhesions (IUA) frequently occur after infectious or mechanical injury to the endometrium, which may lead to infertility and/or pregnancy complications. There are few effective treatments due to the complex function of endometrium and shortage of native materials. 17β-estradiol (E 2 ) is commonly used as an ancillary treatment in IUA patients, but it is limited by its poor solubility in aqueous solutions and low concentrations at the injured sites. In this research, a mini-endometrial curette was used to injure the rat’s endometrium to form an IUA model. 17β-estradiol was encapsulated into the micelles of heparin-poloxamer and a thermosensitive hydrogel (E 2 -HP hydrogel) was formed. This sustained releasing system was applied to restore the structure and function of the injured uterus. E 2 -HP hydrogel was constructed and relevant characteristics including gelation temperature and micromorphology were evaluated. Sustained release of 17β-estradiol from HP hydrogel was performed both in vitro and in vivo. Ultrasonography measurement and pathologic characteristics on the IUA rats were performed to evaluate the therapeutic effect of E 2 -HP hydrogel. Endoplasmic reticulum (ER) stress-related apoptosis was analyzed to explore the possible mechanisms in IUA recovery. E 2 -HP hydrogel showed a prolonged release of E 2 at the targeting region and more effective endometrium regeneration in IUA rats. Significant improvements in both gland numbers and fibrosis area were observed in the E 2 -HP hydrogel group. We also demonstrated that E 2 -HP hydrogel in the recovery of IUA was closely related to the suppression of ER stress signals via the activation of downstream signals, PI3K/Akt and ERK1/2. HP hydrogel might be an effective approach to deliver E 2 into the injured endometrium. Therapeutic strategies targeting ER stress using E 2 -HP hydrogel might be a promising solution for the treatment of women with intrauterine adhesions.

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“…315 Negligible cell toxicity of in vitro toxicity test was detected when 23%, 25% P407 and urokinase were used. [40].…”

Section: Discussionmentioning

confidence: 99%

Hyaluronic Acid on the Urokinase Sustained Release with a Hydrogel System Composed of Poloxamer 407

Hsieh¹,

Lin

Lee³

et al. 2020

Preprint

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Pleural empyema is an inflammatory condition characterized by 35 accumulation of pus inside the pleural cavity, which is usually followed by bacterial pneumonia. During the disease process, the pro-inflammatory and pro-fibrotic cytokines in the purulent pleural effusion cause proliferation of fibroblasts and deposition of extracellular matrix, which lead to fibrin deposition and fibrothorax.Urokinase instillation therapy through a chest drainage tube is frequently used for 40 fibrinolysis in patients with empyema. However, urokinase treatment requires multiple instillation (2-3 times per day, for 4-8 days) and easily flows out from the chest drainage tube due to its high water solubility. In this in vitro study, we developed a thermoresponsive hydrogel based on poloxamer 407 (P407) combined with hyaluronic acid (HA) for optimal loading and release of urokinase. Our results show that the addition 45 of HA to poloxamer gels provides a significantly more compact microstructure, with smaller pore sizes (**p < 0.001). The differential scanning calorimetry (DSC) profile revealed no influence on the micellization intensity of poloxamer gel by HA. The 25% poloxamer-based gel was significantly superior to the 23% poloxamer-based gel, with slower gel erosion when comparing the 16th hour residual gel weight of both gels (*p 50 < 0.05; **p < 0.001). The 25% poloxamer-HA gel also exhibited a superior urokinase release profile and longer release time. A Fourier-transform infrared spectroscopy (FT-IR) study of the P407/HA hydrogel showed no chemical interactions between P407 and HA in the hydrogel system. The thermoresponsive P407/HA hydrogel may have a promising potential in the loading and delivery of hydrophilic drugs. On top of that, in 55 vitro toxicity test of this combination demonstrates a lower toxicity. 60 65

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Poloxamer 407/188 binary thermosensitive hydrogels as delivery systems for infiltrative local anesthesia: Physico-chemical characterization and pharmacological evaluation

Cited by 94 publications

References 41 publications

Thermogelling properties of purified poloxamer 407

Thermogelling properties of purified poloxamer 407

Three-dimensional structure micelles of heparin-poloxamer improve the therapeutic effect of 17β-estradiol on endometrial regeneration for intrauterine adhesions in a rat model

Hyaluronic Acid on the Urokinase Sustained Release with a Hydrogel System Composed of Poloxamer 407

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Poloxamer 407/188 binary thermosensitive hydrogels as delivery systems for infiltrative local anesthesia: Physico-chemical characterization and pharmacological evaluation

Cited by 94 publications

References 41 publications

Thermogelling properties of purified poloxamer 407

Thermogelling properties of purified poloxamer 407

Three-dimensional structure micelles of heparin-poloxamer improve the therapeutic effect of 17&beta;-estradiol on endometrial regeneration for intrauterine adhesions in a rat model

Hyaluronic Acid on the Urokinase Sustained Release with a Hydrogel System Composed of Poloxamer 407

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Three-dimensional structure micelles of heparin-poloxamer improve the therapeutic effect of 17β-estradiol on endometrial regeneration for intrauterine adhesions in a rat model