Co-solubilization of poorly soluble drugs by micellization and complexation

Rao, Venkatramana M.; Nerurkar, Maneesh J.; Pinnamaneni, Swathi; Rinaldi, Frank; Raghavan, Krishnaswamy

doi:10.1016/j.ijpharm.2006.03.042

Cited by 35 publications

(21 citation statements)

References 22 publications

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“…For such a poorly soluble drug, the single approach of micellization seems to be not enough to improve the aqueous solubility to the desirable extent [27], its combination with other solubilisation approaches being necessary. Both RM β CD (5% w/v) and ethanol (20% v/v) (Table 3) enhanced β LAP solubilisation to a great extent.…”

Section: Resultsmentioning

confidence: 99%

Temperature-Sensitive Gels for Intratumoral Delivery ofβ-Lapachone: Effect of Cyclodextrins and Ethanol

Cunha-Filho

Alvarez‐Lorenzo

Martínez‐Pacheco

et al. 2012

The Scientific World Journal

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This work evaluated the potential of Pluronics (varieties F127 and P123) in combination with solubilizing agents to be used as syringeable in situ gelling depots of intratumoral β-lapachone (βLAP). Pluronic dispersions prepared at various concentrations in the absence and the presence of ethanol and randomly methylated β-cyclodextrin (RMβCD) were characterized regarding their rheological properties, drug solubilization capacity, and in vitro release. Pluronic F127 (18–23%) formulations combined high ability to solubilize βLAP (enhancement solubility factor up to 50), adequate gel temperature range (over 25°C), and gel strength at 37°C enough to guarantee the permanence of the formulation in the administration site for a period of time. βLAP release rate was finely tuned by the concentration of the polymer and the addition of RMβCD (diffusion coefficient ranging between 9 and 69 μg·cm−2). The ethanol increases βLAP release rate but simultaneously led to weak gels. This paper shows that βLAP formulations involving temperature-reversible Pluronic gels may be suitable for intratumoral drug delivery purposes.

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Section: Resultsmentioning

confidence: 99%

Temperature-Sensitive Gels for Intratumoral Delivery ofβ-Lapachone: Effect of Cyclodextrins and Ethanol

Cunha-Filho

Alvarez‐Lorenzo

Martínez‐Pacheco

et al. 2012

The Scientific World Journal

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“…[3] Thus, one of the major current challenges facing the pharmaceutical industry involves the development of strategies to improve the aqueous solubility and dissolution rate of drugs. [4][5][6] Drug solubility can be enhanced using traditional approaches such as designing prodrug, [7] reducing particle size by micronization, [8] co-solubilization by micellization and complexation, [9] solid dispersions, [10] and use of solubilizing excipients. [11] Recently, major research efforts have been focused on the development of nanotechnology-based drug delivery systems including biodegradable polymeric nanoparticles, [12] smart polymeric micelles, [13] nanocrystals [14] or nanosuspension, [15] and nanoemulsion [16] to enhance the dissolution rate of poorly soluble drugs and improve oral bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Simvastatin-loaded PLGA nanoparticles for improved oral bioavailability and sustained release: Effect of formulation variables

Soni¹,

Dandagi²,

Gadad³

et al. 2011

Asian J Pharm

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T he objective of this study was to prepare a nanoparticulate formulation of simvastatin (SV) for improving oral bioavailability and sustaining the drug release while investigating the effect of various formulation parameters on characteristics of nanoparticles. Nanoparticles containing SV were prepared by a modified emulsification solvent evaporation technique using a biodegradable polymer, poly(d,l-lactide-coglycolide) (PLGA) as a sustained release carrier. The effect of various formulation parameters such as drug polymer ratios (SV:PLGA, 1:4 to 1:1), organic solvents (methanol/dichloromethane), and surfactants (PVA/polysorbate-80) in a fixed concentration (0.5%, w/v) were studied for particle size, drug loading, and entrapment efficiency. Nanoparticles were characterized by differential scanning calorimetry (DSC) and their shapes were observed by scanning electron microscopy (SEM). An aqueous solubility study indicated that the dissolution rates were remarkably increased for nanoparticles compared with the drug alone. The in vitro drug release study of the nanoparticles showed a biphasic release pattern: one initial burst release of 40.56% in the first 4 h which can be helpful to improve the penetration of drug followed by a second slow-release phase (extended release) consistent with a Higuchi diffusion mechanism. The hypolipidemic activity of nanoparticles was determined in comparison with SV in male Wistar rats for changes in total cholesterol (CH) and triglyceride (TG) levels in blood. Nanoparticles showed a significantly better in vivo performance than SV in reducing total CH and TG levels which is primarily attributed to the improved solubility and dissolution of nanoparticles. Together, these results indicate that nanoparticulate formulations are ideal carriers for oral administration of SV having great potential to improve the oral bioavailability and sustain the drug release, thereby minimizing the dose-dependent adverse effects and maximizing the patient's compliance.

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“…Various techniques can be applied for enhancement of the solubility and dissolution rate of poorly water soluble drugs such as solubilization by cosolvents (11), salt formation (12), inclusion complex in cyclodextrins (13), solid dispersions (14)(15)(16), and micellization (17,18). For chrysin, enhancement of its water solubility by cosolvents has been reported (19).…”

Section: Introductionmentioning

confidence: 99%

Development of chrysin loaded poloxamer micelles and toxicity evaluation in fish embryos

Sassa-deepaeng

Pikulkaew

Okonogi

2016

DD&T

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Co-solubilization of poorly soluble drugs by micellization and complexation

Cited by 35 publications

References 22 publications

Temperature-Sensitive Gels for Intratumoral Delivery ofβ-Lapachone: Effect of Cyclodextrins and Ethanol

Temperature-Sensitive Gels for Intratumoral Delivery ofβ-Lapachone: Effect of Cyclodextrins and Ethanol

Simvastatin-loaded PLGA nanoparticles for improved oral bioavailability and sustained release: Effect of formulation variables

Development of chrysin loaded poloxamer micelles and toxicity evaluation in fish embryos

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