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Poloxamer 407-Based Thermosensitive Emulgel as a Novel Formulation Providing a Controlled Release of Oil-Soluble Pharmaceuticals-Ibuprofen Case Study.

ABSTRACT: This article covers the design and evaluation of a novel drug vehicle: a thermosensitive, injectable, high-oil-content (50% w/w) emulgel providing a controlled release of lipophilic pharmaceuticals. Different vegetable (castor, canola, olive, peanut, grapeseed, linseed), mineral (paraffin) and semisynthetic (isopropyl myristate, oleic acid) oils were screened for ibuprofen (IBU) solubility and for their capacity for high-shear emulsification in a 17% (w/w) aqueous solution of poloxamer 407. Chosen emulgels were subject to a rheological evaluation, a syringeability test (TA.XT texture analyser; 2 mL syringe; 18 G, 20 G and 22 G needles) and a drug release study (48 h; cellulose membrane; 0.05 mol/L phosphate buffer at pH 7.4). Castor oil turned out to be an optimal component for IBU incorporation. Blank and drug-loaded castor oil emulgels were susceptible to administration via a syringe and needle, with the absolute injection force not exceeding 3 kg (29.4 N). The drug release test revealed dose-dependent, quasi-linear kinetics, with up to 44 h of controlled, steady, linear release. The results indicate the significant potential of high-oil-content, oil-in-water thermosensitive emulgel formulations as vehicles for the controlled release of lipophilic APIs.

SUBMITTER: Grela KP

PROVIDER: S-EPMC8658182 | biostudies-literature |

REPOSITORIES: biostudies-literature

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Poloxamer 407 and Hyaluronic Acid Thermosensitive Hydrogel-Encapsulated Ginsenoside Rg3 to Promote Skin Wound Healing.

Project description:Ginsenoside Rg3 has shown beneficial effects in various skin diseases. The current interest in designing and developing hydrogels for biomedical applications continues to grow, inspiring the further development of drug-loaded hydrogels for tissue repair and localized drug delivery. The aim of the present study was to develop an effective and safe hydrogel (Rg3-Gel), using ginsenoside Rg3, and we evaluated the wound-healing potential and therapeutic mechanism of Rg3-Gel. The results indicated that the optimized Rg3-Gel underwent discontinuous phase transition at low and high temperatures. Rg3-Gel also exhibited good network structures, swelling water retention capacity, sustainable release performance, and excellent biocompatibility. Subsequently, the good antibacterial and antioxidant properties of Rg3-Gel were confirmed by in vitro tests. In full-thickness skin defect wounded models, Rg3-Gel significantly accelerated the wound contraction, promoted epithelial and tissue regeneration, and promoted collagen deposition and angiogenesis. In addition, Rg3-Gel increased the expression of autophagy proteins by inhibiting the MAPK and NF-KB pathways in vivo. It simultaneously regulated host immunity by increasing the abundance of beneficial bacteria and the diversity of the wound surface flora. From these preliminary evaluations, it is possible to conclude that Rg3-Gel has excellent application potential in wound-healing drug delivery systems.

| S-EPMC9294355 | biostudies-literature

Amino-functionalized poloxamer 407 with both mucoadhesive and thermosensitive properties: preparation, characterization and application in a vaginal drug delivery system.

Project description:Lack of mucoadhesive properties is the major drawback to poloxamer 407 (F127)-based in situ hydrogels for mucosal administration. The objective of the present study was to construct a novel mucoadhesive and thermosensitive in situ hydrogel drug delivery system based on an amino-functionalized poloxamer for vaginal administration. First, amino-functionalized poloxamer 407 (F127-NH2) was synthesized and characterized with respect to its micellization behavior and interaction with mucin. Then using acetate gossypol (AG) as model drug, AG-loaded F127-NH2-based in situ hydrogels (NFGs) were evaluated with respect to rheology, drug release, ex vivo vaginal mucosal adhesion, in vivo intravaginal retention and local irritation after vaginal administration to healthy female mice. The results show that F127-NH2 is capable of forming a thermosensitive in situ hydrogel with sustained drug release properties. An interaction between positively charged F127-NH2 and negatively charged mucin was revealed by changes in the particle size and zeta potential of mucin particles as well as an increase in the complex modulus of NFG caused by mucin. Ex vivo and in vivo fluorescence imaging and quantitative analysis of the amount of AG remaining in mouse vaginal lavage all demonstrated greater intravaginal retention of NFG than that of an unmodified F127-based in situ hydrogel. In conclusion, amino group functionalization confers valuable mucoadhesive properties on poloxamer 407.

| S-EPMC5595263 | biostudies-literature

The poloxamer P-407 chronic hyperlipidemia mouse model

2006-11-22 | GSE6305 | GEO

Mucosal Applications of Poloxamer 407-Based Hydrogels: An Overview.

Project description: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.

| S-EPMC6161217 | biostudies-other

Chitosan Nanoparticles Loaded Poloxamer 407 Gel for Transungual Delivery of Terbinafine HCl.

Project description:The current study aimed to develop chitosan nanoparticles (CSNP) loaded poloxamer 407 (P407) gel formulation for transungual delivery of terbinafine HCl (TBN). TBN-CSNP were prepared by nanoprecipitation method and optimized by face-centered central composite design (FCCCD). Optimized TBN-CSNP formulation exhibited a spherical shape with hydrodynamic diameter; zeta potential and entrapment efficiency (EE) of 229 ± 5 nm; 37 ± 1.5 mV; and 75 ± 2% respectively. The solid state of TBN and its compatibility with formulation ingredients were confirmed through XRD and FTIR analysis respectively. TBN-CSNP loaded P407 gel exhibited pseudoplastic rheological behavior having a spreadability of 11 ± 2 g·cm/s. The washability study showed that 40 ± 2% of the gel was eroded after washing 12 times. Drug release from TBN-CSNP- and TBN-CSNP-loaded gel was 84 ± 5% and 57 ± 3%, respectively. The cumulative quantity of TBN permeated from TBN-CSNP-loaded P407 gel and TBN-loaded P407 gel was 25 ± 8 and 27 ± 4 µg/cm2, respectively. The nail uptake study showed that 3.6 ± 0.7 and 2.1 ± 0.3 µg of rhodamine was uptaken by the nail following 2 h topical application of TBN-CSNP loaded P407 gel and TBN loaded P407 gel, respectively. Hence, the developed CSNP-based P407 gel formulation can be a potential carrier for transungual delivery of TBN to topically treat onychomycosis.

| S-EPMC9698022 | biostudies-literature

Role of Surfactant Micellization for Enhanced Dissolution of Poorly Water-Soluble Cilostazol Using Poloxamer 407-Based Solid Dispersion via the Anti-Solvent Method.

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| S-EPMC8148127 | biostudies-literature

Electromagnetic field-assisted cell-laden 3D printed poloxamer-407 hydrogel for enhanced osteogenesis.

Project description:3D bioprinted hydrogel has gained enormous attention, especially in tissue engineering, owing to its attractive structure and excellent biocompatibility. In this study, we demonstrated that 3D bioprinted cell-laden 'thermoresponsive' poloxamer-407 (P407) gels have the potential to stimulate osteogenic differentiation of apical papilla stem cells (SCAPs) under the influence of low voltage-frequency (5 V-1 Hz, 0.62 mT) electromagnetic fields (EMFs). SCAPs were initially used for cell-laden 3D printing to biomimic the apical papilla of human teeth. The developed hydrogel exhibited higher mechanical strength as well as good printability, showing high-quality micro-architecture. Moreover, the as-printed hydrogels (5 mm × 5 mm) were loaded with plasminogen activator inhibitor-1 (PAI-1) for testing the combined effect of PAI-1 and EMFs on SCAP differentiation. Interestingly, the 3D hydrogels showed improved viability and differentiation of SCAPs under EMFs' influence as examined by live/dead assay and alizarin Red-S staining, respectively. Therefore, our results confirmed that P407 hydrogels are non-toxic for encapsulation of SCAPs, yielding high cell viability and accelerate the cell migration potential. The 3D hydrogels with PAI-1 exhibited high mRNA expression levels for osteogenic/odontogenic gene markers (ALP, Col-1, DSPP, and DMP-1) vis-à-vis control after 14 days of in vitro culture. Our findings suggest that 3D bioprinted P407 hydrogels are biocompatible for SCAP encapsulation, and the applied low voltage-frequency EMFs could effectively improve dental tissue regeneration, particularly for oral applications.

| S-EPMC9033958 | biostudies-literature

3D Printing of Poloxamer 407 Nanogel Discs and Their Applications in Adjuvant Ovarian Cancer Therapy.

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| S-EPMC7357236 | biostudies-literature

Rutin-Loaded Poloxamer 407-Based Hydrogels for In Situ Administration: Stability Profiles and Rheological Properties.

Project description:Rutin is a flavone glycoside contained in many plants, and exhibits antioxidant, anti-inflammatory, anticancer, and wound-healing properties. The main disadvantage related to the use of this molecule for pharmaceutical application is its poor bioavailability, due to its low solubility in aqueous media. Poloxamer 407-hydrogels show interesting thermo-sensitive properties that make them attractive candidates as pharmaceutical formulations. The hydrophobic domains in the chemical structure of the copolymer, a polymer made up of two or more monomer species, are useful for retaining poorly water-soluble compounds. In this investigation various poloxamer 407-based hydrogels containing rutin were developed and characterized as a function of the drug concentration. In detail, the Turbiscan stability index, the micro- and dynamic rheological profiles and in vitro drug release were investigated and discussed. Rutin (either as a free powder or solubilized in ethanol) did not modify the stability or the rheological properties of these poloxamer 407-based hydrogels. The drug leakage was constant and prolonged for up to 72 h. The formulations described are expected to represent suitable systems for the in situ application of the bioactive as a consequence of their peculiar versatility.

| S-EPMC7352531 | biostudies-literature

Transcription profiling of mouse poloxamer P-407 chronic hyperlipidemia mouse model

Project description:We performed a systemic study of the poloxamer P-407-induced chronic hyperlipidemia in C57BL/6J mice. Mice were treated 96 days every third day.The poloxamer mostly elevates plasma triglycerides and cholesterol while change of the liver cholesterol is not significant. Experiment Overall Design: A group of 12 mice were administered 0.5 g/kg poloxamer P-407 by intraperitoneal (i.p.) injection (poloxamere group), a control group of 4 mice were injected every third day with normal saline. Total RNA from P-407 treated 12 mice has been pooled into 3 biological replicas (Smpl1, Smpl2 and Smpl3). Reference total RNA has been obtained by pooling 4 mice from control group. Each RNA sample has been splitted and hybridised in parallel on cDNA (G4104A) and oligonucleotide (G4120A) mouse microarrays (Agilent Technologies, CA, USA.

2008-06-14 | E-GEOD-6305 | biostudies-arrayexpress

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