Mixed micelle formation with hydrophobic and hydrophilic Pluronic block copolymers: Implications for controlled and targeted drug delivery

Kulthe, Sushant; Inamdar, Nazma; Choudhari, Yogesh; Shirolikar, Seema; Borde, Lalit; Mourya, Vishnukant

doi:10.1016/j.colsurfb.2011.08.002

Cited by 137 publications

(68 citation statements)

References 37 publications

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“…The hydrodynamic diameter 12 and the polydispersity index (PDI) of LX-loaded mixed polymeric nanomicellar systems were determined by photon correlation spectroscopy (PCS) that analyzes the fluctuations in light scattering owing to the Brownian movement of particles. The nanomicellar system was diluted (10 times) with bidistilled water and was placed into a quartz cuvette at 25°C±0.5°C, at 90° to the incident beam using a Zetasizer Nano ZS (Malvern Instruments Ltd., Worcester-shireMalvern, UK).…”

Section: Preparation Of Polymeric Nanomicellar Systemsmentioning

confidence: 99%

Therapeutic effects of lornoxicam-loaded nanomicellar formula in experimental models of rheumatoid arthritis

Helmy¹,

El-Sahar²,

Sayed³

et al. 2017

IJN

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Background Rheumatoid arthritis (RA) is a chronic inflammatory disease treated by nonsteroidal anti-inflammatory drugs (NSAIDs) including lornoxicam (LX). Nanocarriers have been used to increase the efficacy and reduce the side effects of various drugs. The objective of the present study was to compare the therapeutic efficacy of systemic administration of lornoxicam-loaded nanomicellar formula (LX-NM) with that of free LX. Materials and methods The LX-loaded mixed polymeric nanomicellar formula was prepared by direct equilibrium technique. Two rat models were used in the study: carrageenan-induced acute edema and Freund’s complete adjuvant (FCA)-induced chronic arthritis. Results The inhibitory effect of LX-NM on carrageenan-induced edema was higher than free LX for the same dose (1.3 mg/kg, i.p.). LX-NM (0.325 mg/kg, i.p.) produced effects comparable to that of diclofenac, which served as a standard. In the FCA model, daily treatment with LX-NM (0.325 mg/kg, i.p.) starting on day 14 significantly reduced the percentage of edema and increased weight growth. However, the same dose of LX failed to confer any significant change. Additionally, LX-NM significantly attenuated the rise of tumor necrosis factor-α (TNF-α), interleukin-1β, prostaglandin E2, nuclear factor-κβ, malondialdehyde and nitric oxide serum levels. In contrast, LX failed to show any significant reduction in elevated serum biomarkers except for TNF-α. Conclusion LX-NM is an alternative delivery system that is simply prepared at low costs. It showed a superior therapeutic efficacy against RA compared to free LX. Thus, LX-NM can be considered as a promising candidate for treatment of RA and similar inflammatory disorders.

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Section: Preparation Of Polymeric Nanomicellar Systemsmentioning

confidence: 99%

Therapeutic effects of lornoxicam-loaded nanomicellar formula in experimental models of rheumatoid arthritis

Helmy¹,

El-Sahar²,

Sayed³

et al. 2017

IJN

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“…The mixing of P123 and F127 is studied in this work to overcome the limitations of low solubilisation capacity and combine the advantages of high stability of Pluronics These results were expected, as discussed by Lee et al [8] and Kulthe et al [19] , which the Pluronics  mixtures are good solubilising agents of hydrophobic drugs, where the increase in the encapsulated efficiency by the micelles it was observed for mixtures which had a higher ratio of hydrophobic polymer. Supporting our values of S CP to PF mixtures where this behavior still keep the high solubilisation capacity to mixtures that have higher rates of P123 [8,19,21] .…”

Section: Solubilisationmentioning

confidence: 50%

“…Supporting our values of S CP to PF mixtures where this behavior still keep the high solubilisation capacity to mixtures that have higher rates of P123 [8,19,21] . In studies with a series of E M P N E M copolymers was observed the influence of temperature on solubilisation capacity [21] .…”

Section: Solubilisationmentioning

confidence: 52%

“…Copolymers used as solubilizing agents should be mostly micellized in dilute aqueous solution. Low CMC values of surfactants are interesting for drug solubilisation because they provide high stability of their micelles in solutions upon dilution in the blood [7,12,18,19] . Figure 2b shows CMC values of P123, F127 and their mixtures at 25 and 37 °C.…”

Section: Critical Micelle Concentration (Cmc)mentioning

confidence: 99%

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Binary mixture micellar systems of F127 and P123 for griseofulvin solubilisation

et al. 2015

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Sbstract Pluronics molecules self-assemble in aqueous solution providing a core/shell architecture that improves the solubility of hydrophobic drugs. Binary mixtures of Pluronics  have been studied as drug nanocarriers in order to combine their advantages, like high colloidal stability, small particle size and good solubilisation capacity (S cp ). In this work we studied Pluronics  binary mixture, P123 and F127, as nanocarriers of the hydrophobic drug griseofulvin. P123 (E 21 P 67 E 21 ) shows a relative good S cp , whereas F127 (E 98 P 67 E 98 ) shows a good colloidal stability. According to data, these binary mixtures form stables nano-sized comicelles in aqueous solution. The S cp of the P123/F127 systems at 25 and 37 °C was monitored by UV/Visible spectroscopy, showing good results at both temperatures, as would be expected, since P123/F127 have similar length hydrophobic block. Hydrophobic-dependence and temperature-responsive of the systems were evaluated by CMC, particle size and colloidal stability. Hence, stables P123/F127 comicelles may have potencial as hydrophobic drug delivery.

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“…14 However, F68 has a high critical micelle concentration (CMC) and a low drug loading (DL) capacity, resulting in poor dilution stability of the micelles. 14,17 In order to overcome the drawbacks of F68 micelles, a number of methods have been proposed, including appropriate chemical modifications and mixed micelles. 13,18 Vitamin E succinate (α-tocopheryl succinate, VES), a hydrophobic vitamin analog of vitamin E, displays hydrophobicity mainly due to the relatively bulky lipophilic portion in its structure, which makes it more applicable for drug solubilization.…”

mentioning

confidence: 99%

Vitamin E succinate-conjugated F68 micelles for mitoxantrone delivery in enhancing anticancer activity

Liu¹,

Xu²,

Wu³

et al. 2016

IJN

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Mitoxantrone (MIT) is a chemotherapeutic agent with promising anticancer efficacy. In this study, Pluronic F68-vitamine E succinate (F68-VES) amphiphilic polymer micelles were developed for delivering MIT and enhancing its anticancer activity. MIT-loaded F68–VES (F68–VES/MIT) micelles were prepared via the solvent evaporation method with self-assembly under aqueous conditions. F68–VES/MIT micelles were found to be of optimal particle size with the narrow size distribution. Transmission electron microscopy images of F68–VES/MIT micelles showed homogeneous spherical shapes and smooth surfaces. F68–VES micelles had a low critical micelle concentration value of 3.311 mg/L, as well as high encapsulation efficiency and drug loading. Moreover, F68–VES/MIT micelles were stable in the presence of fetal bovine serum for 24 hours and maintained sustained drug release in vitro. Remarkably, the half maximal inhibitory concentration (IC 50 ) value of F68–VES/MIT micelles was lower than that of free MIT in both MDA-MB-231 and MCF-7 cells (two human breast cancer cell lines). In addition, compared with free MIT, there was an increased trend of apoptosis and cellular uptake of F68–VES/MIT micelles in MDA-MB-231 cells. Taken together, these results indicated that F68–VES polymer micelles were able to effectively deliver MIT and largely improve its potency in cancer therapy.

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Mixed micelle formation with hydrophobic and hydrophilic Pluronic block copolymers: Implications for controlled and targeted drug delivery

Cited by 137 publications

References 37 publications

Therapeutic effects of lornoxicam-loaded nanomicellar formula in experimental models of rheumatoid arthritis

Therapeutic effects of lornoxicam-loaded nanomicellar formula in experimental models of rheumatoid arthritis

Binary mixture micellar systems of F127 and P123 for griseofulvin solubilisation

Vitamin E succinate-conjugated F68 micelles for mitoxantrone delivery in enhancing anticancer activity

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