The micellar properties of the poly(oxyethylene) - poly(oxypropylene) copolymer Pluronic F127 in water and electrolyte solution

Attwood, David; Collett, John; Tait, C.J.

doi:10.1016/0378-5173(85)90197-8

Cited by 182 publications

(103 citation statements)

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“…It is known that PF-127 formulations lead to enhanced solubilization of poor water-soluble drugs and a prolonged release profile in many routes of administration. Due to its micellar nature, the PF-127 gels may turn into viscous isotropic liquid crystal gels (67). At low temperatures, the liquid micellar phase is stable and the drug is probably released by diffusion through the extramicellar water channels of the gel matrix (69).…”

Section: Discussionmentioning

confidence: 99%

A Novel Transdermal Delivery System for the Anti-Inflammatory Lumiracoxib: Influence of Oleic Acid on In Vitro Percutaneous Absorption and In Vivo Potential Cutaneous Irritation

2010

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Abstract. Transdermal delivery of non-steroidal anti-inflammatory drugs may be an interesting strategy for delivering these drugs to the diseased site, but it would be ineffective due to low skin permeability. We investigated whether oleic acid (OA), a lipid penetration enhancer in poloxamer gels named poloxamer-based delivery systems (PBDS), can improve lumiracoxib (LM) delivery to/through the skin. The LM partition coefficient (K) studies were carried out in order to evaluate the drug lipophilicity grade (K octanol/buffer ), showing values >1 which demonstrated its high lipophilicity. Both in vitro percutaneous absorption and skin retention studies of LM were measured in the presence or absence of OA (in different concentrations) in PBDS using porcine ear skin. The flux of in vitro percutaneous absorption and in vitro retention of LM in viable epidermis increased in the presence of 10.0% (w/w) OA in 25.0% (w/w) poloxamer gel. In vivo cutaneous irritation potential was carried out in rabbits showing that this formulation did not provide primary or cumulative cutaneous irritability in animal model. The results showed that 25.0% poloxamer gel containing 10.0% OA is potential transdermal delivery system for LM.KEY WORDS: in vitro skin permeation; lumiracoxib; oleic acid; poloxamer-based delivery systems; skin delivery.

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Section: Discussionmentioning

confidence: 99%

A Novel Transdermal Delivery System for the Anti-Inflammatory Lumiracoxib: Influence of Oleic Acid on In Vitro Percutaneous Absorption and In Vivo Potential Cutaneous Irritation

2010

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“…This is a nontoxic block polymer with a molecular weight of 13 500 that exhibits reversible thermal gelation. 17 At low temperature, PF127 exists as micellar subunits in solution, and with an increase in temperature it undergoes micellar swelling, forming a cross-linked network 18 that is capable of protecting protein drugs from degradation. 10 …”

Section: Release Of Spantide II From Gel Formulations Through Synthetmentioning

confidence: 99%

In vitro and in vivo evaluation of topical formulations of Spantide II

et al. 2005

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The purpose of this study was to develop and evaluate topical formulations of Spantide II, a neurokinin-1 receptor (NK-1R) antagonist, for the treatment of inflammatory skin disorders. Spantide II lotion and gel was formulated with and without n-methyl-2-pyrrolidone (NMP) as a penetration enhancer. The release of Spantide II from gels was evaluated using microporous polyethylene and polypropylene membranes in a Franz Diffusion cell setup. In vitro percutaneous absorption of Spantide II from lotion and gel formulations was evaluated using the above setup by replacing the membranes with hairless rat skin. The in vivo anti-inflammatory activity of Spantide II formulations was evaluated in an allergic contact dermatitis (ACD) mouse model. Among different gels studied, PF127 gel showed highest (70-fold) release of Spantide II compared with hydroxypropyl methylcellulose (HPMC) and hydroxypropyl cellulose (HPC) gels. Lotion and gel formulations with or without NMP showed no detectable levels of Spantide II in the receiver compartment of the Franz diffusion cell until 24 hours. However, Spantide II showed significant retention in epidermis and dermis from lotion and gel formulations at 24 hours. The dermal levels increased~3.5-and 2-fold when the lotion and gel formulations contained NMP as compared with the formulation with no NMP (P G .05). The in vivo studies indicated that Spantide II formulations with NMP were effective in significantly reducing ACD response, similar to dexamethasone (0.5 mM). In conclusion, Spantide II was stable as a topical formulation and delivered to target skin tissue (epidermis and dermis) for the treatment of ACD. In addition this study supports the role of cutaneous neurosensory system in modulating inflammatory responses in the skin.

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“…This may be due to the presence of a fewer number of micelles per unit volume in B2, in addition to the extensive hydrating effect of HPMC in this base. 22,30 This combined effect might be the main reason why the gel of B2 did not solidify under the conditions of the experiment.…”

mentioning

confidence: 99%

“…However, the involvement of other mechanisms, including diffusion of the drug through extramicellar aqueous channels, degradation of the gel matrix, or diffusion out of the nanosuspended particles, cannot be excluded. 21,22,30 The 25% pluronic gel with the MC base (B6) was shown to have the highest correlation between cumulative drug release with percentage weight of dissolved gel (r 2 . 0.99).…”

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confidence: 99%

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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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The micellar properties of the poly(oxyethylene) - poly(oxypropylene) copolymer Pluronic F127 in water and electrolyte solution

Cited by 182 publications

References 4 publications

A Novel Transdermal Delivery System for the Anti-Inflammatory Lumiracoxib: Influence of Oleic Acid on In Vitro Percutaneous Absorption and In Vivo Potential Cutaneous Irritation

A Novel Transdermal Delivery System for the Anti-Inflammatory Lumiracoxib: Influence of Oleic Acid on In Vitro Percutaneous Absorption and In Vivo Potential Cutaneous Irritation

In vitro and in vivo evaluation of topical formulations of Spantide II

Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats

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