Development of in vitro-in vivo correlation of parenteral naltrexone loaded polymeric microspheres

Andhariya, Janki V.; Shen, Jie; Choi, Stephanie; Wang, Yan; Zou, Yuan; Burgess, Diane J.

doi:10.1016/j.jconrel.2017.03.396

Cited by 84 publications

(31 citation statements)

References 30 publications

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“…The BUP-loaded microsphere (MS/BUP) was prepared via an oil-in-water emulsion-solvent evaporation method, according to a previous protocol with minor modification 13 . Briefly, PLGA (100.0 mg) and BUP (100.0 mg) were dissolved in 2.0 mL of DCM.…”

Section: Methodsmentioning

confidence: 99%

“…A variety of sustained-release formulations, including microspheres 7 , microgels 8 , Gels 9 , nanoparticles 10 , liposomes 11 , and solid lipid nanoparticles 12 , have been investigated to extend the duration of analgesia induced by local anesthetics. Recently, the poly(lactic- co -glycolic acid) microspheres (PLGA MSs) have gained in popularity due to their excellent biodegradability, biocompatibility, and stable physicochemical properties during manufacturing and storage 13 , 14 . PLGA MSs have been successfully loaded with lidocaine 15 , bupivacaine 16 , ropivacaine 17 , and other local anesthetics, achieving nerve blockade durations of 6-24 h. However, the poor in situ properties of MSs and the initial burst release of drugs can reduce blockade duration, and result in local and systemic toxicity 16 , 18 .…”

Section: Introductionmentioning

confidence: 99%

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Precision-guided long-acting analgesia by hydrogel-immobilized bupivacaine-loaded microsphere

Zhang¹,

Cong²,

Xu³

et al. 2018

Theranostics

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Peripheral nerve blockade (PNB) is a conventional strategy for the management of acute postoperative pain. However, the short duration of the associated analgesia and the potential systemic toxicity due to the low molecular weights of local anesthetics limit their application.Methods: An in situ forming injectable Gel-microsphere (Gel-MS) system consisting of PLGA-PEG-PLGA Gel (Gel) and Gel-immobilized bupivacaine-loaded microsphere (MS/BUP) was prepared for precision-guided long-acting analgesia. A series of in vitro characterizations, such as scanning electron microscopy, rheology analysis, confocal laser scanning microscopy, drug release, and erosion and degradation, were carried out. After that, the in vivo analgesia effect of the Gel-MS system, the immobilization effect of Gel on the MS, and biocompatibility of the system were evaluated using a sciatic nerve block model.Results: The BUP release from the Gel-MS system was regulated by both the inner MS and the outer Gel matrix, demonstrating sustained BUP release in vitro for several days without an initial burst release. More importantly, incorporation of the Gel immobilized the MS and hindered the diffusion of MS from the injection site because of its in situ property, which contributed to a high local drug concentration and prevented systemic side effects. In vivo, a single injection of Gel-MS/BUP allowed rats to maintain sensory and motor blockade significantly longer than treatment with MS/BUP (P < 0.01) or BUP-loaded Gel (Gel-BUP, P < 0.01). Histopathological results demonstrated the excellent biodegradability and biocompatibility of the Gel-MS system without neurotoxicity.Conclusion: This precision-guided long-acting analgesia, which provides an in situ and sustained release of BUP, is a promising strategy for long-acting analgesia, and could represent a potential alternative for clinical pain management.

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Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Precision-guided long-acting analgesia by hydrogel-immobilized bupivacaine-loaded microsphere

Zhang¹,

Cong²,

Xu³

et al. 2018

Theranostics

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“…Most of these products are based on the use of poly(lactic‐co‐glycolic) acid‐based polymers. As such, the FDA has conducted extensive research on characterizing these products to begin to build out a weight of evidence approach that will be effective for this class of products and support the development of in vitro / in vivo correlations . The FDA has linked this advanced characterization with PBPK research into computational methods to predict the performance of long‐acting injectables and quantitative clinical pharmacology (QCP) research into more efficient in vivo study designs.…”

Section: Equivalence Of Complex Mixtures and Formulationsmentioning

confidence: 99%

Innovation for Generic Drugs: Science and Research Under the Generic Drug User Fee Amendments of 2012

Lionberger¹

2019

Clin Pharma and Therapeutics

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Regulatory science is science and research intended to improve decision making in a regulatory framework. Improvements in decision making can be in both accuracy (making better decisions) and in efficiency (making faster decisions). Science and research supported by the Generic Drug User Fee Amendments of 2012 (GDUFA) have focused on two innovative methodologies that work together to enable new approaches to development and review of generic drugs: quantitative models and advanced in vitro product characterization. Quantitative models faithfully represent current scientific understanding. They are tools pharmaceutical scientists and clinical pharmacologists use for making better and faster product development decisions. Advances in the in vitro product comparisons provide the measurements of product differences that are the critical input into the models. This paper outlines four areas where science and research funded by GDUFA support synergistic use of models and characterization at critical decision points during generic drug product development and review.

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“…The IVIVC (polynomial linear model) was also developed with the two-stage Wagner-Nelson method. Other studies also indicate that in many cases the Wagner-Nelson equation is used for obtaining the absorption data, which is then plotted against dissolution data and processed in a linear regression, logistic, or polynomial manner (11)(12)(13)(14)(15)(16)(17)(18). Next, the satisfactory results in terms of a correlation coefficient and convoluted in vivo data are presented; although, in most cases no external validation is done.…”

Section: Deconvolutionmentioning

confidence: 99%

In Vitro-In Vivo Correlation (IVIVC): From Current Achievements Towards the Future

Tuszyński¹,

Szlęk²,

Polak³

et al. 2018

Dissolution Technol.

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Conventional in vitro-in vivo correlation (IVIVC) based on compendial dissolution testing faces many obstacles, among which are problems in establishing meaningful correlation for immediate release dosage forms, lack of intravenous data in cases of many drugs without a possibility to obtain a unit impulse response, and well-known difficulties to build an IVIVC model for BCS III and BCS IV class drugs. Three major elements are obligatory for IVIVC development: in vitro dissolution data, in vivo pharmacokinetic profile, and modeling tools. Dissolution testing and modeling approaches are under heavy development to create predictive IVIVIC/IVIVR models. Application of noncompendial dissolution methods, biorelevant media, and equipment simulating the human gastrointestinal tract, together with sophisticated multivariate statistical methods and mechanistic approaches, are nominated to be the future of IVIVC.

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Development of in vitro-in vivo correlation of parenteral naltrexone loaded polymeric microspheres

Cited by 84 publications

References 30 publications

Precision-guided long-acting analgesia by hydrogel-immobilized bupivacaine-loaded microsphere

Precision-guided long-acting analgesia by hydrogel-immobilized bupivacaine-loaded microsphere

Innovation for Generic Drugs: Science and Research Under the Generic Drug User Fee Amendments of 2012

In Vitro-In Vivo Correlation (IVIVC): From Current Achievements Towards the Future

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