Pluronic® F127 gel formulations of Deslorelin and GnRH reduce drug degradation and sustain drug release and effect in cattle

Wenzel, J. G. W.; Balaji, K S Sree; Koushik, Kavitha; Navarre, Christine B.; Duran, Sue H.; Rahe, C.H.; Kompella, Uday B.

doi:10.1016/s0168-3659(02)00271-7

Cited by 103 publications

(57 citation statements)

References 23 publications

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“…For these reasons Poloxamer gels have been considered for short-term therapies like pain management [49], infection treatment [48,50], and fertility control [51].…”

Section: Pharmaceutical Applicationmentioning

confidence: 99%

Thermosensitive Self-Assembling Block Copolymers as Drug Delivery Systems

et al. 2011

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Self-assembling block copolymers (poloxamers, PEG/PLA and PEG/PLGA diblock and triblock copolymers, PEG/polycaprolactone, polyether modified poly(Acrylic Acid)) with large solubility difference between hydrophilic and hydrophobic moieties have the property of forming temperature dependent micellar aggregates and, after a further temperature increase, of gellifying due to micelle aggregation or packing. This property enables drugs to be mixed in the sol state at room temperature then the solution can be injected into a target tissue, forming a gel depot in-situ at body temperature with the goal of providing drug release control. The presence of micellar structures that give rise to thermoreversible gels, characterized by low toxicity and mucomimetic properties, makes this delivery system capable of solubilizing water-insoluble or poorly soluble drugs and of protecting labile molecules such as proteins and peptide drugs.

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“…For these reasons Poloxamer gels have been considered for short-term therapies like pain management [49], infection treatment [48,50], and fertility control [51].…”

Section: Pharmaceutical Applicationmentioning

confidence: 99%

Thermosensitive Self-Assembling Block Copolymers as Drug Delivery Systems

et al. 2011

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“…Pluronics have been cited in the literature as being used as hydrophilic thermosensitive polymers for sustaining the action of many hydrophilic drugs given by injection, such as interleukin-2, 19 recombinant human growth hormone, 20 and deslorelin. 21 Pluronics are a family of commercially available block copolymers with variable surface properties. Pluronic F127, also known as poloxamer 407, is an ABA block copolymer formed of poly(oxyethylene) units (70%) referred to as A and poly(oxypropylene) blocks (30%) referred to as B, 22 which undergo a thermogelation phenomenon upon increasing temperatures.…”

Section: Introductionmentioning

confidence: 99%

Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats

Salem¹

2010

IJN

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Abstract:The production of an intramuscular (IM) injection of natural progesterone would provide a safer solution than using semi synthetic progesterone. However, disadvantages such as low solubility and a short half life prevent the use of natural progesterone. In this study, we formulated a sustained release form of natural progesterone to be given as IM injection. A progesterone nanosuspension (PNS) was first developed and then dispersed in a thermosensitive gel matrix. The selected nanoparticles showed an average particle size of 267 nm and a zeta potential approaching-41 mV. The in vitro release profile of PNS from the F127 plus methyl cellulose gel followed zero order kinetics and correlated linearly with the weight percentage of gel dissolved, demonstrating that the overall rate of release of PNS is controlled by dissolution of the pluronic F127/methyl cellulose (MC) gel (r 2 . 0.99). The pharmacokinetic parameters of the PNS (6 mg/mL) in pluronic F127/MC gel were evaluated in comparison with the control progesterone suspension. After the administration of PNS in F127/MC gel into the rats, a maximum serum concentration of 22.1 ± 1.9 ng/mL was reached at a T max of 4.05 ± 0.1 h. The terminal half life was 12.7 ± 0.8 h. The area under the curve AUC 0-∞ of the injected formula was 452.75 ± 42.8 ng·h/mL and the total mean residence time was 18.57 ± 1.44 h. The PNS in gel was significantly different from the control in rate and extent at P , 0.001. The natural progesterone which was nanosized and formulated in a thermosensitive gel significantly sustained the action of natural progesterone so that it could be injected every 36 h instead of every day. Moreover, this formula is expected to provide a much safer choice than the use of semi-synthetic progesterone.

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“…It gels at room temperature and has mostly been used in controlled-release drug delivery (Barichello et al, 1999;Desai and Blanchard, 2000;El Kamel, 2002;Wenzel et al, 2002). However, it has previously been applied as part of a scaffold for rat neural progenitor cells in a model of neurotrauma (Vacanti et al, 2001) and as a construct to support the growth and differentiation of lung progenitor cells (Cortiella et al, 2006).…”

Section: Introductionmentioning

confidence: 99%

Compatibility of human fetal neural stem cells with hydrogel biomaterials in vitro

et al. 2008

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Stroke and spinal cord or brain injury often result in cavity formation. Stem cell transplantation in combination with tissue engineering has the potential to fill such a cavity and replace lost neurons. Several hydrogels containing unique features particularly suitable for the delicate nervous system were tested by determining whether these materials were compatible with fetal human neural stem cells (hNSCs) in terms of toxicity and ability to support stem cell differentiation in vitro. The hydrogels examined were pluronic F127 (PF127), Matrigel and PuraMatrix. We found that PF127, in a gelated (30%) form, was toxic to hNSCs, and Matrigel, in a gelated (1-50%) form, prevented hNSCs' normal capacity for neuronal differentiation. In contrast, PuraMatrix was the most optimal hydrogel for hNSCs, since it showed low toxicity when gelated (0.25%) and retained several crucial properties of hNSCs, including migration and neuronal differentiation. Further optimization and characterization of PuraMatrix is warranted to explore its full potential in assisting neural regeneration in vivo.

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Pluronic® F127 gel formulations of Deslorelin and GnRH reduce drug degradation and sustain drug release and effect in cattle

Cited by 103 publications

References 23 publications

Thermosensitive Self-Assembling Block Copolymers as Drug Delivery Systems

Thermosensitive Self-Assembling Block Copolymers as Drug Delivery Systems

Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats

Compatibility of human fetal neural stem cells with hydrogel biomaterials in vitro

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