In vitro-in vivo correlation of parenteral risperidone polymeric microspheres

Shen, Jie; Choi, Stephanie; Qu, Wen; Wang, Yan; Burgess, Diane J.

doi:10.1016/j.jconrel.2015.09.051

Cited by 101 publications

(35 citation statements)

References 34 publications

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“…Because in vitro-in vivo correlation of drug released from lactide-co-glycolide polymeric has been determined definitely and systematically. These evidences were showed in studies by D'Souza et al (2014) and Shen et al (2015). The blood concentration of amifostine in AM treated mice should be much lower than that of IV injection of amifostine solution.…”

Section: In Vitro Kinetics Of Amifostine Release From Plga Microspheresmentioning

confidence: 80%

Sustained-release microspheres of amifostine for improved radio-protection, patient compliance, and reduced side effects

Jin

2016

Drug Delivery

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A biweekly administration of sustained-release microsphere dosage form of amifostine, a radioprotective drug used in radiotherapy, was performed to examine the feasibility to minimize injection frequency and blood concentration-associated side effects. Model animal trials indicated that this subcutaneously injecting microspheres, 50-100 mm in diameter, achieved bi-weekly prolonged radio-protective efficacy and, at the same time, significantly reduced skin irritation than the solution form of amifostine given by the same administration route. In addition, the hypertension associated with blood concentration of amifostine was not observed in the drug-treated rats. The animals given the amifostine microspheres and amifostine showed significantly differences in white blood cell, red blood cell, hematocrit, hemoglobin and spleen tissue histopathology after exposed under a cobalt-60 g-radiation at a dose rate of 1.0 Gy/min for 6 min. The in vitro release profile of amifostine from the micropsheres showed a minor initial burst (less than 20% of total drug loading in the first day of administration), consisting with the side effects observations. The results suggest that amifostine encapsulated in sustained-release microspheres may be an ideal dosage form for prolonged radio-protective efficacy and improved patient compliance.

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Section: In Vitro Kinetics Of Amifostine Release From Plga Microspheresmentioning

confidence: 80%

Sustained-release microspheres of amifostine for improved radio-protection, patient compliance, and reduced side effects

Jin

2016

Drug Delivery

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“…As shown in Fig. 3, both in vitro release methods investigated were able to discriminate compositionally equivalent risperidone microsphere formulations with similar particle size but different inner structures/porosity (Shen et al, 2015). Formulation 1 had a higher burst release percentage (ca.…”

Section: In Vitro Release Characteristics Of Risperidone Microspheresmentioning

confidence: 88%

A reproducible accelerated in vitro release testing method for PLGA microspheres

Shen

Lee

Choi

et al. 2016

International Journal of Pharmaceutics

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The objective of the present study was to develop a discriminatory and reproducible accelerated in vitro release method for long-acting PLGA microspheres with inner structure/porosity differences. Risperidone was chosen as a model drug. Qualitatively and quantitatively equivalent PLGA microspheres with different inner structure/porosity were obtained using different manufacturing processes. Physicochemical properties as well as degradation profiles of the prepared microspheres were investigated. Furthermore, in vitro release testing of the prepared risperidone microspheres was performed using the most common in vitro release methods (i.e. sample-andseparate and flow through) for this type of product. The obtained compositionally equivalent risperidone microspheres had similar drug loading but different inner structure/porosity. When microsphere particle size appeared similar, porous risperidone microspheres showed faster microsphere degradation and drug release compared with less porous microspheres. Both in vitro release methods investigated were able to differentiate risperidone microsphere formulations with differences in porosity under real-time (37°C) and accelerated (45°C) testing conditions. Notably, only the accelerated USP apparatus 4 method showed good reproducibility for highly porous risperidone microspheres. These results indicated that the accelerated USP apparatus 4 method is an appropriate fast quality control tool for long-acting PLGA microspheres (even with porous structures). Graphical Abstract*

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“…These polymer systems present a diversity of amphiphilic character, degradation rate, and physical characteristics. Also, they are easily prepared, allowing achievement of the desired requirements for a prolonged therapeutic effect of the drug, increasing the effectiveness of the treatment [91].…”

Section: Polyesters Useful In Drug Delivery Systemsmentioning

confidence: 99%