Nifedipine solid dispersion in microparticles of ammonio methacrylate copolymer and ethylcellulose binary blend for controlled drug deliveryEffect of drug loading on release kinetics

Huang, Jingjun; Wigent, Rodney J.; Bentzley, Catherine M.; Schwartz, Joseph B.

doi:10.1016/j.ijpharm.2006.03.035

Cited by 77 publications

(44 citation statements)

References 28 publications

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“…After 1 d of incubation, 68.1 wt% of drug was released from microspheres prepared with 5 wt% of daidzein, compared to 45 wt% of drug released from microspheres prepared with 10 wt% of daidzein. A similar phenomenon has also been reported in previous studies, 33,34 and a possible reason is that lower drug loading leads to relatively more drug being located in the region close to the surface of the microspheres. 33 The drug release mechanism from microspheres prepared by emulsification solvent evaporation involves two main processes: (i) an initial burst release of drug located close to microsphere surfaces, (ii) a relatively constant drug release stage depending on drug diffusion and microsphere degradation.…”

Section: Daidzein Release Profilessupporting

confidence: 87%

Multilayered drug delivery coatings composed of daidzein-loaded PHBV microspheres embedded in a biodegradable polymer matrix by electrophoretic deposition

Chen

Yao

et al. 2016

J. Mater. Chem. B

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The development of drug delivery coating systems for local and long-term drug release is gaining increasing interest especially to functionalize bioinert implants with osseointegration and antibacterial properties. In this study, a biodegradable drug delivery coating platform consisting of drug-loaded PHBV microspheres embedded in an alginate-PVA matrix was fabricated by a one-step electrophoretic deposition (EPD) process. Layer by layer (LbL) deposition was exploited to generate chitosan-alginate multilayers on the EPD-produced coating to enlarge the diffusional barrier around the microspheres for controlled drug release. Daidzein, selected as a model drug due to its anti-osteoporosis properties, was pre-encapsulated in PHBV microspheres. The parameters for microsphere fabrication were optimized by an orthogonal design approach. The loading efficiency of daidzein in both the microspheres and in the deposited coatings was adjusted by varying the processing parameters during microsphere fabrication and the EPD process. The degradation of the deposited multilayers was investigated in PBS for up to 14 days. The degradation rate, surface roughness and wettability, as well as adhesion strength of the coatings during degradation were evaluated by applying a range of techniques. A controlled and sustained daidzein release was detected from both free microspheres and microsphere-containing coatings. Finally cytotoxicity and stimulatory effects of daidzein or daidzein-loaded coatings, on both MC3T3-E1 and RAW264.7 cell lines, were studied to validate the potential of the developed coatings for orthopedic applications.

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Section: Daidzein Release Profilessupporting

confidence: 87%

Multilayered drug delivery coatings composed of daidzein-loaded PHBV microspheres embedded in a biodegradable polymer matrix by electrophoretic deposition

Chen

Yao

et al. 2016

J. Mater. Chem. B

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“…Consequently, the solubility behavior of a class II drug is the key determinant of its oral bioavailability (2). To date, a considerable number of drugs need to be administered frequently a day because of their short half-life in the body, which results in a significant fluctuation in the plasma drug concentration and drug toxic side effects (3). Therefore, the development of a sustainedrelease oral dosage form instead of the conventional preparations for the side effect reduction and patient compliance improvement is desirable.…”

Section: Introductionmentioning

confidence: 99%

“…Several approaches have been investigated to solve the aforementioned problems, including (a) combining solubilization technology, e.g., solid dispersion, with sustained-release techniques, e.g., a membrane-controlled tablet, and (b) polydisperse systems, e.g., self-microemulsion and nanoparticle (3,4). This method (a) would thus result in a more complex manufacturing process, and careful control of each step would be required to produce reproducible and reliable preparations (5).…”

Section: Introductionmentioning

confidence: 99%

Improved Bioavailability of Poorly Water-Soluble Drug Curcumin in Cellulose Acetate Solid Dispersion

et al. 2011

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Abstract. Curcumin (Cur), one of the most widely used natural active constituents with a great variety of beneficial biological and pharmacological activities, is a practically water-insoluble substance with a short biologic half-life. The aim of this study was to develop a sustained-release solid dispersion by employing water-insoluble carrier cellulose acetate for solubility enhancement, release control, and oral bioavailability improvement of Cur. Solid dispersions were characterized by solubility, in vitro drug release, Fourier transform infrared spectroscopy, X-ray diffractometry, and differential scanning calorimetry studies. The in vivo performance was assessed by a pharmacokinetic study. Solid-state characterization techniques revealed the amorphous nature of Cur in solid dispersions. Solubility/ dissolution of Cur was enhanced in the formulations in comparison with pure drug. Sustained-release profiles of Cur from the solid dispersions were ideally controlled in vitro up to 12 h. The optimized formulation provided an improved pharmacokinetic parameter (C max =187.03 ng/ml, t max =1.95 h) in rats as compared with pure drug (C max =87.06 ng/ml, t max =0.66 h). The information from this study suggests that the developed solid dispersions successfully enhanced the solubility and sustained release of poorly water-soluble drug Cur, thus improving its oral bioavailability effectively.

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“…In the course of the non-solvent addition, the drug and carrier are co-precipitated to form microparticles. At the end, the resulted microparticle suspension is filtered and dried 58 .…”

Section: Solvent Evaporation Methodmentioning

confidence: 99%

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2010

IJPSR

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The solubility behavior of drugs remains one of the most challenging aspects in the formulation development. Although there was a great interest in solid dispersion systems during the past four decades to increase solubility by improving dissolution rate and bioavailability of poorly soluble drugs; there commercial use has been very limited, primarily because of manufacturing difficulties and various stability problems. It can be carried out by reducing drug particle size to the absolute minimum, and hence improving drug wet-ability, bioavailability may be significantly improved. Solid dispersion of drugs was generally produced by melt or solvent evaporation methods. Recently, surfactants have been included to stabilize the formulations, thus avoiding drug recrystallization and potentiating their solubility. New manufacturing processes to obtain solid dispersions have also been developed to reduce the drawbacks of the initial process. In this review, it is intended to discuss the eminent approach to improve the solubility or the dissolution rate and recent revival has been discussed.

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Nifedipine solid dispersion in microparticles of ammonio methacrylate copolymer and ethylcellulose binary blend for controlled drug deliveryEffect of drug loading on release kinetics

Cited by 77 publications

References 28 publications

Multilayered drug delivery coatings composed of daidzein-loaded PHBV microspheres embedded in a biodegradable polymer matrix by electrophoretic deposition

Multilayered drug delivery coatings composed of daidzein-loaded PHBV microspheres embedded in a biodegradable polymer matrix by electrophoretic deposition

Improved Bioavailability of Poorly Water-Soluble Drug Curcumin in Cellulose Acetate Solid Dispersion

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