Solid Dispersion Approach to the Formulation of Organic Liquid Drugs Using Polyethylene Glycol 6000 as a Carrier

Chiou, Win L.; Smith, Lloyd D.

doi:10.1002/jps.2600600127

Cited by 14 publications

(3 citation statements)

References 8 publications

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“…In 1950s, Jatzkewitz used polyvinylpyrrolidone, mescaline and peptide to form the first drug carrier via coacervation. After that, polyethylene glycol‐ and dextran‐based polymer drug carriers have gotten lots of attention. Polymer‐based drug carrier had many types, such as microparticle, colloid, and micelle .…”

Section: Introductionmentioning

confidence: 99%

Synthesis of mesoporous silica nanoparticle‐encapsulated alginate microparticles for sustained release and targeting therapy

Liao

2013

J Biomed Mater Res

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This study reports the synthesis of mesoporous silica nanoparticle-encapsulated alginate microparticles (MSN@Alg) for sustained release and targeting therapy. The MSN@Alg was synthesized by air dynamical atomization, and the effects of several critical factors including concentration of alginate solution, flow rate of alginate solution, flow rate of air, the distance between nozzle and calcium bath, and stirring rate of calcium on the particle size of the synthesized MSN@Alg were investigated. For studying the sustained release properties of the MSN@Alg, rhodamine 6G (R6G) was used as a model drug, and we compared the release properties of R6G/MSN and R6G/MSN@Alg using different concentrations of alginate, concentrations and volumes of phosphate-buffered saline (PBS) buffer solutions. The sustained release behavior of the R6G/MSN@Alg system can be prolonged to 20 days with an optimal condition of 1 mg R6G/MSN@Alg to 2 mL PBS (10 mM). To achieve targeting therapy, an anticancer drug, doxorubicin (Dox), was loaded into MSN@Alg, and a arginine, glycine, and aspartic acid (RGD)-based peptide was functionalized onto the surface of MSN@Alg for the purpose of specific targeting. The results showed that the intracellular drug delivery efficiency was greatly enhanced (i.e., 3.5-folds) for the Dox/MSN@Alg-RGD drug delivery system.

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Section: Introductionmentioning

confidence: 99%

Synthesis of mesoporous silica nanoparticle‐encapsulated alginate microparticles for sustained release and targeting therapy

Liao

2013

J Biomed Mater Res

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“…PVP was used to enhance the dissolution rate of a number of drugs such as 5-lipoxygenase inhibitor SB210661 and benidipine HCl [25]. Dissolution of prednisolone has been enhanced by PEG fusion dispersions [26]. Jachowicz and Czech [27] formulated piroxicam solid dispersions containing hydroxypropyl methylcellulose acetate succinate (HPMCAS) as a carrier for ocular delivery.…”

Section: Introductionmentioning

confidence: 99%

Design, Formulation and Evaluation of Piroxicam Capsules Prepared by Solid Dispersion Technique

Swidan

2013

BJPR

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Objective: To improve the dissolution of poorly soluble Piroxicam (PRXM) by solid dispersion technique using water soluble carriers with or without the addition of sodium lauryl sulphate (SLS) as surfactant. Methods and Materials: Solid dispersions of Piroxicam were prepared using different polymers such as polyethylene glycol (PEG 4000 and PEG 6000) polyvinylpyrrolidone (PVP K30 and PVP K90) without or with addition of 2% of (SLS). Solid dispersions were formulated in drug polymer ratios 1:1, 1:2, and 1:4, each ratio without or with 2% SLS using solvent evaporation method. The prepared formulae were assayed for drug content, production yield and stability properties. Dissolution profiles were done in phosphate buffer pH 7.4 and the in vitro release was evaluated according to the % released after 20, 30, 45 and 60 minutes. An accelerated stability study was done over 3 months at 40 o and 60ºC and with relative humidity (RH) 75%. Results and Discussion: All of the formulated solid dispersions displayed better dissolution profiles as compared to the pure drug. Formulae containing 2% SLS displayed

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“…[9] Because DTPA penta-ethyl ester exists as an oily liquid, formulating it in a solid dosage form would be very desirable in terms of ease of packaging, handling and administering. The solid dispersion approach has been used previously [10, 11] ; it allows for a more uniform product than does mechanical mixing of liquids with solids. In addition, solid dispersions of poorly water soluble active pharmaceutical ingredients can increase solubility, dissolution rate and bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Solid dispersions of the penta-ethyl ester prodrug of diethylenetriaminepentaacetic acid (DTPA): formulation design and optimization studies

Pasqua

Zhang

et al. 2013

Pharmaceutical Development and Technology

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The penta-ethyl ester prodrug of diethylenetriaminepentaacetic acid (DTPA), which exists as an oily liquid, was incorporated into a solid dispersion for oral administration by the solvent evaporation method using blends of polyvinylpyrrolidone (PVP), Eudragit® RL PO and α-tocopherol. D-optimal mixture design was used to optimize the formulation. Formulations that had a high concentration of both Eudragit® RL PO and α-tocopherol exhibited low water absorption and enhanced stability of the DTPA prodrug. Physicochemical properties of the optimal formulation were evaluated using Fourier transform infrared (FTIR) spectroscopy and differential scanning calorimetry (DSC). In vitro release of the prodrug was evaluated using the USP Type II apparatus dissolution method. DSC studies indicated that the matrix had an amorphous structure, while FTIR spectrometry showed that DTPA penta-ethyl ester and excipients did not react with each other during formation of the solid dispersion.. Dissolution testing showed that the optimized solid dispersion exhibited a prolonged release profile, which could potentially result in a sustained delivery of DTPA penta-ethyl to enhance bioavailability. In conclusion, DTPA penta-ethyl ester was successfully incorporated into a solid matrix with high drug loading and improved stability compared to prodrug alone.

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Solid Dispersion Approach to the Formulation of Organic Liquid Drugs Using Polyethylene Glycol 6000 as a Carrier

Cited by 14 publications

References 8 publications

Synthesis of mesoporous silica nanoparticle‐encapsulated alginate microparticles for sustained release and targeting therapy

Synthesis of mesoporous silica nanoparticle‐encapsulated alginate microparticles for sustained release and targeting therapy

Design, Formulation and Evaluation of Piroxicam Capsules Prepared by Solid Dispersion Technique

Solid dispersions of the penta-ethyl ester prodrug of diethylenetriaminepentaacetic acid (DTPA): formulation design and optimization studies

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