Poloxamers, poloxamines and polymeric micelles: Definition, structure and therapeutic applications in cancer

Pluronics (tri-block copolymers) have a significant role in the pharmaceutical industry and are being used to enhance the solubility and delivery of hydrophobic drugs in different marketed formulations. However, instability and unsatisfactory drug-loading capacity are the major weak spots of these pluronic micelles. The present research work is designed to solve the existing issues by the solubilization study of hydrophobic drugs in different pluronic micelles at variable temperatures. The solubilization of the hydrophobic antiepileptic drug lamotrigine (LAM) in five different pluronic micelles viz. P84, P85, F127, F108, and F68 was studied at different temperatures, 37, 47, and 57 °C, using UV–visible spectroscopy. The solubilization of LAM in pluronic micelles increased with the increase in temperature. Small-angle neutron scattering (SANS) measurements were used to observe the morphological and structural changes taking place in pluronics by increasing the temperature. The SANS results showed the morphological changes of spherical P84 micelles to prolate ellipsoidal micelles at 57 °C due to remarkable increase in the aggregation number. This morphological conversion was further confirmed by the heat transfer method (HTM) and dynamic light scattering (DLS) measurements. DLS measurements confirmed that LAM-loaded micelles showed a greater hydrodynamic diameter ( D h ) compared to unloaded micelles, assuring LAM solubilization in the pluronic micelles. The rate of controlled release of LAM from five different pluronic micelles was accessed by using different kinetic models to evaluate the in vitro release profile. This is the first report in which HTM measurements are established for the analysis of morphological changes in the thermoresponsive pluronic micelles in real time. The present work corroborates how we can control the drug-loading capacity, morphological structure of the drug carrier, as well as drug release by simply changing the temperature of pluronic micellar media.

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“…Accordingly, P84, having a 60% PPO content which is relatively higher than other pluronics under study, displayed the highest DLE. 34,35…”

Section: Results and Discussionmentioning

confidence: 99%

Temperature-Dependent Solubilization of the Hydrophobic Antiepileptic Drug Lamotrigine in Different Pluronic Micelles—A Spectroscopic, Heat Transfer Method, Small-Angle Neutron Scattering, Dynamic Light Scattering, and in Vitro Release Study

et al. 2019

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“…Poloxamers have an amphiphilic character with both association and adsorption properties and improve solubilization and stabilization of compounds as a result of their notable physiological properties and low toxicity [37]. Poloxamers and poloxamines are non-ionic surfactants that have diverse applications in various biomedical fields such as drug delivery, medical imaging, as well as cancer therapy [38]. In a previous work, it was found that an increase of concentration of poloxamer 407 produces a reduction of both particle size and PDI [17].…”

Section: Resultsmentioning

confidence: 99%

Ultrasound-Assisted Encapsulation of Sacha Inchi (Plukenetia volubilis Linneo.) Oil in Alginate-Chitosan Nanoparticles

et al. 2019

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Sacha inchi oil is rich in essential and non-essential fatty acids and other types of bioactive agents like tocopherols and polyphenolic compounds, which are very well-known antioxidants. In this study, the encapsulation of sacha inchi oil in alginate (AL) and chitosan (CS) nanoparticles was achieved with the assistance of high-intensity ultrasound. Nanoemulsion is the most effective delivery and high stability system for lipophilic bioactive agents. Chitosan and surfactant concentrations were varied to study their effect on particle formulations. Size, zeta-potential, polydispersity, and stability of particles were determined in time to optimize the preparation conditions. Sacha inchi oil encapsulated in AL-CS nanoparticles showed a higher loading efficiency and stability for short and long periods compared with other vegetable oils such as olive and soybean. Also, because of the types of tocopherols present in sacha inchi oil (γ- and δ-tocopherols), a much higher antioxidant activity (95% of radical reduction in 15 min) was found in comparison with nanocapsules with olive oil, which contain α-tocopherols. The particles showed high efficiency of protein loading at high concentration of bovine serum albumin (BSA) and a low rate of leaching profiles in various testing media like simulated gastric and intestinal fluids with/without enzymes, that is, pepsin 0.1% (w/v) and pancreatin 0.1% (w/v), respectively.

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“…Further application strategies with poloxamer regard cancer therapy [4]. Poloxamers have gained interest in the field of oncology because of their ability to developed stable systems with the capability of efficient drugs encapsulation and deliver.…”

Section: Poloxamer As Micellar Systemsmentioning

confidence: 99%

“…Poloxamers and poloxamines are examples of these LCGT biocompatible thermoreversible hydrogels that were introduced in the 1950s by BASF (Iselin, NJ, USA) when they started being used for detergent development, but also in other areas, like agriculture, food, and paints [4].…”

Section: Introductionmentioning

confidence: 99%

Poloxamer Hydrogels for Biomedical Applications

2019

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This review article focuses on thermoresponsive hydrogels consisting of poloxamers which are of high interest for biomedical application especially in drug delivery for ophthalmic, injectable, transdermal, and vaginal administration. These hydrogels remain fluid at room temperature but become more viscous gel once they are exposed to body temperature. In this way, the gelling system remains at the topical level for a long time and the drug release is controlled and prolonged. Poloxamers are synthetic triblock copolymers of poly(ethylene oxide)-b-poly(propylene oxide)-b-poly(ethylene oxide) (PEO-PPO-PEO), also commercially known as Pluronics®, Synperonics® or Lutrol®. The different poloxamers cover a range of liquids, pastes, and solids, with molecular weights and ethylene oxide–propylene oxide weight ratios varying from 1100 to 14,000 and 1:9 to 8:2, respectively. Concentrated aqueous solutions of poloxamers form thermoreversible gels. In recent years this type of gel has arouse interest for tissue engineering. Finally, the use of poloxamers as biosurfactants is evaluated since they are able to form micelles in an aqueous environment above a concentration threshold known as critical micelle concentration (CMC). This property is exploited for drug delivery and different therapeutic applications.

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Poloxamers, poloxamines and polymeric micelles: Definition, structure and therapeutic applications in cancer

Cited by 119 publications

References 77 publications

Temperature-Dependent Solubilization of the Hydrophobic Antiepileptic Drug Lamotrigine in Different Pluronic Micelles—A Spectroscopic, Heat Transfer Method, Small-Angle Neutron Scattering, Dynamic Light Scattering, and in Vitro Release Study

Temperature-Dependent Solubilization of the Hydrophobic Antiepileptic Drug Lamotrigine in Different Pluronic Micelles—A Spectroscopic, Heat Transfer Method, Small-Angle Neutron Scattering, Dynamic Light Scattering, and in Vitro Release Study

Ultrasound-Assisted Encapsulation of Sacha Inchi (Plukenetia volubilis Linneo.) Oil in Alginate-Chitosan Nanoparticles

Poloxamer Hydrogels for Biomedical Applications

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