Academic literature on the topic 'Pluronic Lecithin Organogel (PLO gel)'

Skin aging is one of the prominent problems associated with skin as each part of body ages with the time, skin is the external organ where the sign and symptoms of aging are readily evident. However cosmetics as well as pharmaceutical approaches delayed skin aging. Gel are best fitted in all these essential criteria because of their excellent appearance, smoothness, desired consistency, fast drug release, ease of manufacturing and quality assessment and admirable stability. Recently gel formulation have been modified to yield an advance drug delivery system known as ―organogels‖. Gel define as a semi-solid preparation having an external solvent phase, apolar [organogel] or polar [hydrogel] immobilized within the space available of a three dimensional network structure. Lecithin is a natural surfactant isolated from eggs or soya bean, when it combined with water and non-polar solvent, it form gels. PLO gels have gained importance in recent years as transdermal drug delivery system. It is a thermodynamically stable, visco-elastic system, which is non-irritating, odorless and biodegradable. Pluronic F127 or poloxamer is a copolymer of polyoxyethylene and polyoxypropylene which forms a thermoreversible gel in concentrations between 15-30%w/v. Water plays the role of a structure-forming agent and stabilizes the process of gel formation as it solubilizes the pluronic and other hydrophilic drugs. PLO gel system facilitates the delivery of hydrophilic as well as lipophilic drugs owing to the presence of both oil and aqueous phases within the gel system.

9531 Background: Chemotherapy induced peripheral neuropathy (CIPN) is a prevalent dose limiting toxicity for several important cancer treatment agents. CIPN can impair function and cause distress. There are no proven pharmacologic treatments for established CIPN currently. This double blind randomized placebo controlled trial evaluated a compounded topical gel for this problem. The novelty of this treatment is that it might incorporate several agents with different mechanisms of action to provide relief locally without negative systemic effects. Methods: Patients with CIPN (rated ≥4 out of 10) for at least one month, related to previous and/or concurrent exposure to neurotoxic agents, were randomized to baclofen 10 mg, amitriptyline HCL 40 mg and ketamine 20 mg in a pluronic lecithin organogel (BAK-PLO) vs placebo (PLO) to determine its effect on numbness, tingling, pain, and motor function. Exclusion criteria included other causes and/or current treatment for peripheral neuropathy. The primary endpoint was the baseline adjusted sensory subscale of the EORTC QLQ-CIPN20, at 4 weeks. Results: Between February and May 2008, 208 patients were enrolled onto this trial. Four week data are shown in the table below, higher numbers being better. The percentage of patients that had improvements of at least 10, on a 100 point scale, in the motor subscale was statistically significantly higher in the BAK-PLO arm, p=.04. There were no unwanted toxicities associated with the BAK-PLO that were significantly different from placebo and no evidence of CNS or systemic toxicity. Conclusions: Topical treatment with BAK-PLO appears to moderately improve symptoms of CIPN. This topical gel was well tolerated without systemic side effects. [Table: see text] No significant financial relationships to disclose.

2′-hydroxyflavanone (2HF) is a dietary flavonoid with anticancer activity towardsmultiple cancers. Here, we report that topically applied 2HF inhibits the growth of intradermalimplants of melanoma in immunocompetent mice. 2HF induced apoptosis and inhibited the growthof the human SK-MEL-24 as well as murine B16-F0 and B16-F10 melanoma cell lines in vitro.Apoptosis was associated with depletion of caspase-3, caspase-9, and PARP1 in B16-F0 and SKMEL-24 cells. Caspase-9 and MEKK-15 were undetected even in untreated B16-F10 cells. Signalingproteins TNFα, and phospho-PDGFR-β were depleted in all three cell lines; MEKK-15 was depletedby 2HF in SK-MEL-24 cells. 2HF enhanced sunitinib (an MEK and PDGFR-β inhibitor) and AZD2461 (a PARP1 inhibitor) cytotoxicity. 2HF also depleted the Ral-regulated, stress-responsive,antiapoptotic endocytic protein RLIP76 (RALBP1), the inhibition of which has previously beenshown to inhibit B16-F0 melanoma growth in vivo. Functional inhibition of RLIP76 was evidentfrom inhibition of epidermal growth factor (EGF) endocytosis by 2HF. We found that topicallyapplied 2HF–Pluronic Lecithin Organogel (PLO) gel inhibited B16-F0 and B16-F10 tumorsimplanted in mice and caused no overt toxicity despite significant systemic absorption. 2HFtreatment reduced phospho-AKT, vimentin, fibronectin, CDK4, cyclinB1, and BCL2, whereas itincreased BIM and phospho-AMPK in excised tumors. Several cancer signals are controlled byendocytosis, a process strongly inhibited by RLIP76 depletion. We conclude that 2HF–PLO gel maybe useful for topical therapy of cutaneous metastases of melanoma and could enhance theantineoplastic effects of sunitinib and PARP1 inhibitors. The mechanism of action of 2HF inmelanoma overlaps with RLI76 inhibitors.

Kaempferia parviflora (KP) extract has been used in the Thai medicinal plant recipe, which the methoxyflavones are the main active compound. These compounds have low water solubility, high lipophilicity, and low bioavailability. The aim of this study was to develop the pluronic lecithin organogel (PLO) and PLO with d-limonene (PLO-L) for enhancing transdermal delivery of KP extract. These formulations were prepared and their physicochemical properties, stability, and in vitro skin permeation were evaluated. For the result, all formulations exhibited good physicochemical properties and stable under storage condition for 3 months. The permeation of KP extract-loaded PLO-L and PLO formulation showed significantly higher total methoxyflavones permeated through the skin than KP extract in water, which PLO-L provided the highest permeated flux of total methoxyflavones. This result suggested that d-limonene play a role as skin permeation enhancer. Organogel consisting of poloxamer 407 and lecithin also increased the skin permeation of KP extract. In conclusion, PLO-L could be a potential transdermal delivery system for KP extract.

Infections due to HSV-1 affect many people all over the world. To counteract this pathology, usually characterized by perioral sores or by less frequent serious symptoms including keratitis, synthetic antiviral drugs are employed, such as acyclovir, often resulting in resistant viral strains under long-term use. Many plant-derived compounds, such as mangiferin and quercetin, have demonstrated antiviral potentials. In this study, smart semisolid forms based on phosphatidylcholine and Pluronic were investigated as delivery systems to administer mangiferin on skin and mucosae affected by HSV-1 infection. Particularly, lecithin organogels, Pluronic gel, and Pluronic lecithin organogels were formulated and characterized. After the selection of gel compositions, physical aspects, such as rheological behavior, spreadability, leakage, and adhesion were evaluated, suggesting a scarce suitability of the lecithin organogel for topical administration. Mangiferin was efficiently included in all type of gels. An in vitro study based on the Franz cell enabled us to find evidence of the gel capability to control drug diffusion, especially in the case of Pluronic organogel, while an in vivo study conducted on human volunteers demonstrated the safeness of all of the gels after cutaneous administration. Furthermore, a plaque reduction assay demonstrated the virucidal effect of mangiferin loaded in a Pluronic gel and a Pluronic lecithin organogel against the HSV-1 KOS strain.

Topical drug treatment aims at providing high concentrations of drugs at the site of application so as to avoid adverse systemic effects associated with oral administration. Smart polymers, or stimuli-responsive polymers, are able to respond to a stimulus by showing physical or chemical changes in their behaviour as, for example, the delivery of the drug carried by them. The thermo-responsive nature of Pluronic® F-127 (Basf, Ludwigshafen, Germany) makes it an excellent candidate for the delivery of drugs at various application sites. In recent years, PF-127, and later, Pluronic lecithin organogels (PLO), have attracted particular interest in the design of dermal and transdermal delivery systems with a view to promoting, improving or retarding drug permeation through the skin, bearing in mind that for topical delivery systems, accumulation in the skin with minimal permeation is desired, while for systemic delivery, the opposite behaviour is preferred. In this review, we discuss the properties and characteristics of PF-127 and Pluronic lecithin organogels (PLO), and present many examples and advantages of the application of these polymeric systems in topical and transdermal administration of drugs. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

Joint pain with high prevalence and yet without any specific treatment option is posing a challenge to healthcare professionals day by day. Amongst several treatment options currently utilized for arthritic joint pain are merely giving symptomatic relief rather than curative treatment. Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most widely accessed treatment option amongst all of the options. However, their adverse effects profile is a major hurdle for their use, especially in elderly patients. The present study was focused on developing a transdermal patch of a novel NSAID Loxoprofen sodium with enhanced penetration and improved patient compliance. Pluronic lecithin organogel (PLO) was selected as transdermal drug delivery platform to enhance its penetration through skin. Moreover, the transdermal route bypasses first-pass metabolism, gastrointestinal (GI) side effects, and the necessity to administer drug orally. All of these credentials ultimately improved patient compliance. Several experimental batches (PL1 to PL8) were formulated to prepare the PLO of loxoprofen sodium. All the batches were evaluated for physical appearance, pH, viscosity, spreadability, drug content, and in vitro drug diffusion profiles. An optimized batch was selected on the basis of the obtained results. It showed sustained drug release up to 12 h. The study evidenced that similar transdermal formulations of other NSAIDs can significantly enhance current treatment scenario for joint pain. Moreover, conversion of such formulations in transdermal patches or other forms ensure sustained and reproducible transdermal flux, which can be further fabricated as bioequivalent to the oral formulations. Further studies can be designed to evaluate the clinical applicability of the formulation.

Conselho Nacional de Pesquisa e Desenvolvimento Científico e Tecnológico - CNPq
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - CAPES
Rutin is a flavonoid widely reported in the literature for its antioxidant properties, anti-inflammatory, vasoprotective, antithrombogen, among others. However, its low solubility in aqueous media reduces its bioavailability orally and, therefore, transdermal administration proves to be promising. Thus, the present work aimed to obtain, characterize and evaluate an activity and antioxidant activity of a gel. PLO (Pluronic Lecithin Organogel) containing rutin for transdermal administration.The analytical methodology for rutin quantification was developed and validated by high performance liquid chromatography (HPLC). Initially it was evaluated as an influence of the concentration of Polaxamer 407, obtained by the extrusion method with the aid of syringes, in front of the centrifugation test. The formulation that remained stable after the test was characterized by partical size determination, in vitro release study, in vitro skin penetration study, in vitro skin adhesion study. Also assessed for stability for 60 days at varying temperatures and at predetermined times, physico-chemical characteristics such as pH, density, viscosity and spreadability, as well as organoleptic characteristics, were evaluated. The antioxidant activity of the formulation was evaluated by the TRAP and TAR methods, comparing it with a positive control, Trolox. The results demonstrate that a formulation with higher concentration of Polaxamer is more stable and that is why it was characterized. The partical size were perfect for dermal administration. The formulation demonstrated controlled release of the drug after 24 hours, being able to permeate as deeper layers of the skin and to be absorbed into the systemic circulation, in addition to good adhesion to the skin surface. During the accelerated stability study, as formulations stored at low temperature, they underwent small variations in density, viscosity and spreadability relative to those stored at room temperature, while the pH remained stable throughout and favorable for application in skin. However, as observed variations were not sufficient to cause visual signs of instability. As for the antioxidant activity, a formulation showed greater activity in relation to the Trolox control and the free rutin, but it was not able to sustain an activity for a longer time, presenting a lower TAR value than Trolox. Thus, a chosen formulation has been shown capable of promoting a permeation of the rutin by transdermal route in a controlled manner, as well as being stable at an ambient temperature and having more significant antioxidant activity than the free rutin, and is therefore promising to administration of rutin by this route.
A rutina é um flavonoide bastante estudado devido principalmente as suas propriedades antioxidantes, anti-inflamatória, vasoprotetora e antitrombogência. No entanto, sua baixa solubilidade em meio aquoso reduz sua biodisponibilidade por via oral e, portanto, a administração por via transdérmica pode ser uma alternativa promissora. Dessa forma, o presente trabalho teve por objetivo obter, caracterizar e avaliar a estabilidade e a atividade antioxidante de um gel contendo Pluronic Lecithin Organogel (PLO) contendo rutina, para administração pela via transdérmica. A metodologia analítica para quantificação de rutina foi desenvolvida e validada por cromatografia líquida de alta eficiência (CLAE). Inicialmente foi avaliado qual a influência da concentração do Polaxamer 407, obtidos pelo método de extrusão com auxílio de seringas, frente ao teste de centrifugação. A formulação que permaneceu estável após o teste foi caracterizada através da determinação do tamanho de partícula, estudo de liberação, penetração cutânea e adesão à pele, todos in vitro. Foi também avaliada a estabilidade do produto durante 60 dias em variadas temperaturas em tempos pré-determinados, além das análises físico-químicas, como pH, densidade, viscosidade e espalhabilidade, bem como características organolépticas. A atividade antioxidante da formulação foi determinada pelos métodos TRAP e TAR, em comparação com um controle positivo, o Trolox. Os resultados demonstraram que a formulação contendo maior concentração de Polaxamer é mais estável e por isso esta foi caracterizada. O tamanho de partícula encontrado foi 4,33 μm e o sistema se mostrou homogêneo, ideal para administração cutânea. A formulação demonstrou liberação controlada do fármaco após 24 horas, sendo capaz de permear as camadas mais profundas da pele e ser absorvida para circulação sistêmica, além de boa adesão à superfície da pele. Durante o estudo de estabilidade acelerada, as formulações armazenadas em baixa e alta temperatura, sofreram pequenas variações na densidade, na viscosidade e na espalhabilidade, em relação àquelas armazenadas a temperatura ambiente, enquanto que o pH se manteve estável durante todo o tempo e favorável à sua aplicação na pele. Além disso, as variações observadas não foram suficientes para provocar alterações visuais de instabilidade. Quanto à atividade antioxidante, a formulação demonstrou maior atividade em relação ao controle Trolox e à rutina livre, porém de forma não duradoura, apresentando valor de TAR menor que o Trolox. Sendo assim, a formulação escolhida, demonstrou-se capaz de promover a permeação da rutina por via transdérmica de forma controlada, bem como estabilidade a temperatura ambiente e com atividade antioxidante significativa, sendo considerada então promissora a administração da rutina por esta via.
São Cristóvão, SE