Evaluation of Selected Micronized Poloxamers as Tablet Lubricants

Desai, Divyakant; Zia, Hossein; Quadir, Anisul

doi:10.1080/10717540701203042

Cited by 16 publications

(5 citation statements)

References 14 publications

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“…Overlay of X-ray diffraction patterns between a ibuprofen and physical mixtures (PM); b ibuprofen and fusion mixtures (FM) this study provides a sophisticated, accurate, and sensitive measurement for the energies required for powders to flow under certain conditions. As can be seen, the BFE values decreased with the polymer content and simple explanation for that is the waxy nature of Poloxamer 407 which acts a lubricant (44), and hence, less energy is required for powder flow. Hausner ratio of 1.25 and higher indicates poor flow, and almost all the formulations along with the drug fell in that range except for FM 1:0.75 which was in the free flowing range which was consistent with rheometer data.…”

Section: Discussionmentioning

confidence: 80%

Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407

2016

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ABSTRACT. Aim of current research was to prepare ibuprofen-poloxamer 407 binary mixtures using fusion method and characterize them for their physicochemical and performance properties. Binary mixtures of ibuprofen and poloxamer were prepared in three different ratios (1:0.25, 1:0.5, and 1:0.75, respectively) using a water-jacketed high shear mixer. In vitro dissolution and saturation solubility studies were carried out for the drug, physical mixtures, and formulations for all ratios in de-ionized water, 0.1 N HCl (pH = 1.2), and phosphate buffer (pH = 7.2). Thermal and physical characterization of samples was done using modulated differential scanning calorimetry (mDSC), X-ray powder diffraction (XRD), and infrared spectroscopy (FTIR). Flow properties were evaluated using a powder rheometer. Maximum solubility enhancement was seen in acidic media for fused formulations where the ratio 1:0.75 had 18-fold increase. In vitro dissolution studies showed dissolution rate enhancement for physical mixtures and the formulations in all three media. The most pronounced effect was seen for formulation (1:0.75) in acidic media where the cumulative drug release was 58.27% while for drug, it was 3.67%. Model independent statistical methods and ANOVA based methods were used to check the significance of difference in the dissolution profiles. Thermograms from mDSC showed a characteristic peak for all formulations with T peak of around 45°C which suggested formation of a eutectic mixture. XRD data displayed that crystalline nature of ibuprofen was intact in the formulations. This work shows the effect of eutectic formation and micellar solubilization between ibuprofen and poloxamer at the given ratios on its solubility and dissolution rate enhancement.

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Section: Discussionmentioning

confidence: 80%

Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407

2016

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“…Poloxamers, like other surfactants, when dispersed in the liquid, at low concentrations, exist individually as monomolecular micelles. But as the concentration of the poloxamer in the system increases, this results in the formation of multimolecular aggregates (22). Polypropylene oxide (PPO) forms central hydrophobic core wherein methyl groups interact via van der Waals forces with substance undergoing solubilisation.…”

Section: General Characteristicsmentioning

confidence: 99%

Pluronic® F-127 and Pluronic Lecithin Organogel (PLO): Main Features and their Applications in Topical and Transdermal Administration of Drugs

et al. 2012

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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.

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“…[5] NCs with high intermolecular lattice energy remain stable in circulation. [6] For cancer patients with the leaky peritumoral vasculature, stable NCs are expected to show more favorable pharmacokinetic (PK) and biodistribution (BD) profiles than commercial formulations, such as Taxol (surfactant-solubilized PTX) and Abraxane (albumin-bound PTX), which circulate as smaller particles such as micelles (14 nm) [7,8] and albumin-bound drugs (≈10 nm), [9,10] respectively.…”

Section: Introductionmentioning

confidence: 99%

A Comparative In Vivo Study of Albumin‐Coated Paclitaxel Nanocrystals and Abraxane

Park

Hedrick

et al. 2018

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Nanoparticulate drug carriers exploit the enhanced permeability of tumor vasculature to achieve selective delivery of chemotherapeutic drugs. For this purpose, nanoparticles (NPs) need to circulate with a long half-life, enter tumors via the permeable vasculature and stay in tumors via favorable interactions with tumor cells. To fulfill these requirements, albumin-coated nanocrystal formulation of paclitaxel (PTX), Cim-F-alb, featuring high drug loading content, physical stability in serum, and surface-bound albumin in its native conformation is prepared. The pharmacokinetic and biodistribution (PK/BD) profiles of Cim-F-alb in a mouse model of B16F10 melanoma show that Cim-F-alb exhibits a longer plasma half-life and a greater PTX deposition in tumors than Abraxane by ~1.5 and ~4.6 fold, respectively. Biolayer interferometry analysis indicates that Cim-F-alb has less interaction with serum proteins than nanocrystals lacking albumin coating, indicating the protective effect of the surface-bound albumin against opsonization in the initial deposition phase. With the advantageous PK/BD profiles, Cim-F-alb shows greater and longer-lasting anti-cancer efficacy than Abraxane at the equivalent dose. This study demonstrates the significance of controlling circulation stability and surface property of NPs in efficient drug delivery to tumors and enhanced anti-cancer efficacy.

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Evaluation of Selected Micronized Poloxamers as Tablet Lubricants

Cited by 16 publications

References 14 publications

Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407

Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407

Pluronic® F-127 and Pluronic Lecithin Organogel (PLO): Main Features and their Applications in Topical and Transdermal Administration of Drugs

A Comparative In Vivo Study of Albumin‐Coated Paclitaxel Nanocrystals and Abraxane

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