Comparison of in vitro–in vivo release of Risperdal® Consta® microspheres

Rawat, Archana; Bhardwaj, Upkar; Burgess, Diane J.

doi:10.1016/j.ijpharm.2012.05.006

Cited by 86 publications

(38 citation statements)

References 22 publications

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“…Elevating temperature can facilitate drug diffusion from the microspheres as well as expedite polymer matrix degradation. It has been shown that accelerated drug release from PLGA microspheres can be achieved under elevated temperature conditions (Rawat et al, 2012; Shen and Burgess, 2012; Zolnik et al, 2006). …”

Section: Introductionmentioning

confidence: 99%

In vitro and in vivo performance of dexamethasone loaded PLGA microspheres prepared using polymer blends

Wang

Burgess

2015

International Journal of Pharmaceutics

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The foreign body reaction is the major cause of the dysfunction and relatively short lifetime associated with implanted glucose biosensors. An effective strategy to maintain sensor functionality is to apply biocompatible coatings that elute drug to counter the negative tissue reactions. This has been achieved using dexamethasone releasing poly (lactic-co-glycolic acid) (PLGA) microspheres embedded in a poly vinyl alcohol (PVA) hydrogel coating. Accordingly, the biosensor lifetime relies on the duration and dose of drug release from the coating. To achieve long-term drug release mixed populations of microspheres have been used. In the current study, microspheres were prepared by blending low (25 KDa) and high (113 KDa) molecular weight PLGA at different mass ratios to overcome problems associated with mixing multiple populations of microspheres. “Real-time” in vitro studies demonstrated dexamethasone release for approximately 5 months. An accelerated method with discriminatory ability was developed to shorten drug release to less than 2 weeks. An in vivo pharmacodynamics study demonstrated efficacy against the foreign body reaction for 4.5 months. Such composite coatings composed of PLGA microspheres prepared using polymer blends could potentially be used to ensure long-term performance of glucose sensors.

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Section: Introductionmentioning

confidence: 99%

In vitro and in vivo performance of dexamethasone loaded PLGA microspheres prepared using polymer blends

Wang

Burgess

2015

International Journal of Pharmaceutics

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“…Briefly, the in vivo plasma profiles of the prepared risperidone PLGA microspheres were deconvoluted using the Loo-Riegelman method [19]. Standard errors are not shown in the deconvoluted in vivo absorption profiles because the average plasma concentration values were used.…”

Section: Development Of An Ivivcmentioning

confidence: 99%

“…However, there is some controversy in the literature with respect to the role of enzymes in PLGA degradation since in vitro assessment cannot be entirely correlated to polymer degradation in vivo [37]. It was also determined that the in vivo risperidone release/ absorption in rabbits was faster than that in humans as reported in the literature (plateaued by day 56 [19]). This can be explained by the interspecies differences in the local in vivo environment (such as interstitial fluid volume and components (e.g.…”

Section: In Vivo Studies Of the Risperidone Microspheresmentioning

confidence: 99%

“…Over the past decades, the development of IVIVCs for parenteral microspheres has increasingly gained more significance. The same principles as detailed in the FDA IVIVC Guidance on extended release oral dosage forms have been applied in literature to develop IVIVCs for parenteral drug products [15][16][17][18][19][20]. However, due to their complex release characteristics (e.g.…”

Section: Introductionmentioning

confidence: 99%

“…bi-or tri-phasic release profiles), deconvolution of in vivo data and correlation with in vitro release data have been challenging. Until now, there are only a few literature reports on the establishment of IVIVCs for parenteral polymeric microspheres, albeit with different in vitro release testing approaches, such as the USP 4 method [19,20], dialysis based methods [17,18], as well as sample-and-separate methods [21][22][23]. None of these has addressed the importance of developing an IVIVC for compositionally equivalent PLGA microspheres with manufacturing differences.…”

Section: Introductionmentioning

confidence: 99%

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In vitro-in vivo correlation of parenteral risperidone polymeric microspheres

Shen

Choi

et al. 2015

Journal of Controlled Release

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The objective of the present study was to determine whether an in vitro-in vivo correlation (IVIVC) can be established for polymeric microspheres that are equivalent in formulation composition but prepared with different manufacturing processes. Risperidone was chosen as a model therapeutic and poly(lactic-co-glycolic acid) (PLGA) with similar molecular weight as that used in the commercial product Risperdal ® Consta ® was used to prepare risperidone microspheres. Various manufacturing processes were investigated to produce the risperidone microspheres with similar drug loading (approx. 37%) but distinctly different physicochemical properties (e.g. porosity, particle size and particle size distribution). In vitro release of the risperidone microspheres was investigated using different release testing methods (such as sampleand-separate and USP apparatus 4). In vivo pharmacokinetic profiles of the risperidone microsphere formulations following intramuscular administration were determined using a rabbit model. Furthermore, the obtained pharmacokinetic profiles were deconvoluted using the LooRiegelman method and the calculated in vivo release was compared with the in vitro release of these microspheres. Level A IVIVCs were established and validated for the compositionally equivalent risperidone microspheres based on the in vitro release data obtained using USP apparatus 4. The developed IVIVCs demonstrated good predictability and were robust. These results showed that the developed USP apparatus 4 method was capable of discriminating PLGA microspheres that are equivalent in formulation composition but with manufacturing differences and predicting their in vivo performance in the investigated animal model.

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In Vitro–In VivoCorrelation for Pharmaceutical Nano‐ and Microsystems

Desai

Patravale

2020

Characterization of Pharmaceutical Nano and Microsystems

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Comparison of in vitro–in vivo release of Risperdal® Consta® microspheres

Cited by 86 publications

References 22 publications

In vitro and in vivo performance of dexamethasone loaded PLGA microspheres prepared using polymer blends

In vitro and in vivo performance of dexamethasone loaded PLGA microspheres prepared using polymer blends

In vitro-in vivo correlation of parenteral risperidone polymeric microspheres

In Vitro–In VivoCorrelation for Pharmaceutical Nano‐ and Microsystems

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