Probing the mechanism of bupivacaine drug release from multivesicular liposomes.

Anesthetics, Local / chemistry Bupivacaine / chemistry Drug Liberation Liposomes Microscopy, Electron, Scanning
Bupivacaine Cryo-SEM IVRT Liposome Multivesicular Reverse dialysis

Journal

Journal of controlled release : official journal of the Controlled Release Society
ISSN: 1873-4995
Titre abrégé: J Control Release
Pays: Netherlands
ID NLM: 8607908

Informations de publication

Date de publication:
28 01 2019
Historique:
received: 11 09 2018
revised: 16 11 2018
accepted: 16 12 2018
pubmed: 24 12 2018
medline: 21 3 2020
entrez: 22 12 2018
Statut: ppublish

Résumé

The mechanism of drug release from complex dosage forms, such as multivesicular liposomes (MVLs), is complex and oftentimes sensitive to the release environment. This challenges the design and development of an appropriate in vitro release test (IVRT) method. In this study, a commercial bupivacaine MVL product was selected as a model product and an IVRT method was developed using a modified USP 2 apparatus in conjunction with reverse-dialysis membranes. This setup allowed the use of in situ UV-Vis probes to continuously monitor the drug concentration during release. In comparison to the traditional sample-and-separate methods, the new method allowed for better control of the release conditions allowing for study of the drug release mechanism. Bupivacaine (BPV) MVLs exhibited distinct tri-phasic release characteristics comprising of an initial burst release, lag phase and a secondary release. Temperature, pH, agitation speed and release media composition were observed to impact the mechanism and rate of BPV release from MVLs. The size and morphology of the MVLs as well as their inner vesicle compartments were analyzed using cryogenic-scanning electron microscopy (cryo-SEM), confocal laser scanning microscopy and laser diffraction, where the mean diameters of the MVLs and their inner "polyhedral" vesicles were found to be 23.6 ± 11.5 μm and 1.52 ± 0.44 μm, respectively. Cryo-SEM results further showed a decrease in particle size and loss of internal "polyhedral" structure of the MVLs over the duration of release, indicating erosion and rearrangement of the lipid layers. Based on these results a potential MVL drug release mechanism was proposed, which may assist with the future development of more biorelevant IVRT method for similar formulations.

Identifiants

DOI: 10.1016/j.jconrel.2018.12.029 PMID: 30576748
pubmed: 30576748
pii: S0168-3659(18)30732-6
doi: 10.1016/j.jconrel.2018.12.029
pii:
doi:

Substances chimiques

Anesthetics, Local 0
Liposomes 0
Bupivacaine Y8335394RO

Types de publication

Journal Article Research Support, U.S. Gov't, Non-P.H.S. Research Support, U.S. Gov't, P.H.S.

Langues

eng

Sous-ensembles de citation

IM

Pagination

279-287

Informations de copyright

Published by Elsevier B.V.

Auteurs

Soumyarwit Manna (S)

Division of Therapeutic Performance, Office of Research and Standards, Office of Generic Drugs, Center for Drug Evaluation and Research, Food and Drug Administration, Silver Spring, MD 20993, USA; Division of Biology, Chemistry and Materials Science, Office of Science and Engineering Laboratories, Center for Devices and Radiological Health, Food and Drug Administration, Silver Spring, MD 20993, USA.

Yong Wu (Y)

Division of Biology, Chemistry and Materials Science, Office of Science and Engineering Laboratories, Center for Devices and Radiological Health, Food and Drug Administration, Silver Spring, MD 20993, USA.

Yan Wang (Y)

Division of Therapeutic Performance, Office of Research and Standards, Office of Generic Drugs, Center for Drug Evaluation and Research, Food and Drug Administration, Silver Spring, MD 20993, USA.

Bonhye Koo (B)

Division of Therapeutic Performance, Office of Research and Standards, Office of Generic Drugs, Center for Drug Evaluation and Research, Food and Drug Administration, Silver Spring, MD 20993, USA; Division of Biology, Chemistry and Materials Science, Office of Science and Engineering Laboratories, Center for Devices and Radiological Health, Food and Drug Administration, Silver Spring, MD 20993, USA.

Lynn Chen (L)

Division of Therapeutic Performance, Office of Research and Standards, Office of Generic Drugs, Center for Drug Evaluation and Research, Food and Drug Administration, Silver Spring, MD 20993, USA; Division of Biology, Chemistry and Materials Science, Office of Science and Engineering Laboratories, Center for Devices and Radiological Health, Food and Drug Administration, Silver Spring, MD 20993, USA.

Peter Petrochenko (P)

Division of Therapeutic Performance, Office of Research and Standards, Office of Generic Drugs, Center for Drug Evaluation and Research, Food and Drug Administration, Silver Spring, MD 20993, USA.

Yixuan Dong (Y)

Division of Product Quality Research, Office of Testing and Research, Office of Pharmaceutical Quality, Center for Drug Evaluation and Research, Food and Drug Administration, Silver Spring, MD 20993, USA.

Stephanie Choi (S)

Division of Therapeutic Performance, Office of Research and Standards, Office of Generic Drugs, Center for Drug Evaluation and Research, Food and Drug Administration, Silver Spring, MD 20993, USA.

Darby Kozak (D)

Division of Therapeutic Performance, Office of Research and Standards, Office of Generic Drugs, Center for Drug Evaluation and Research, Food and Drug Administration, Silver Spring, MD 20993, USA.

Berk Oktem (B)

Division of Biology, Chemistry and Materials Science, Office of Science and Engineering Laboratories, Center for Devices and Radiological Health, Food and Drug Administration, Silver Spring, MD 20993, USA.

Xiaoming Xu (X)

Division of Product Quality Research, Office of Testing and Research, Office of Pharmaceutical Quality, Center for Drug Evaluation and Research, Food and Drug Administration, Silver Spring, MD 20993, USA. Electronic address: xiaoming.xu@fda.hhs.gov.

Jiwen Zheng (J)

Division of Biology, Chemistry and Materials Science, Office of Science and Engineering Laboratories, Center for Devices and Radiological Health, Food and Drug Administration, Silver Spring, MD 20993, USA. Electronic address: jiwen.zheng@fda.hhs.gov.

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Classifications MeSH

questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Agents du système nerveux central › Dépresseurs du système nerveux central › Anesthésiques › Anesthésiques locaux › Probing the mechanism of bupivacaine drug...
questionsmedicales.fr › Composés chimiques organiques › Amines › Dérivés de l'aniline › Anilides › Bupivacaïne › Probing the mechanism of bupivacaine drug...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Pharmacocinétique › Libération de médicament › Probing the mechanism of bupivacaine drug...
questionsmedicales.fr › Technologie, industrie et agriculture › Produits manufacturés › Matériaux biomimétiques › Membrane artificielle › Liposomes › Probing the mechanism of bupivacaine drug...
questionsmedicales.fr › Techniques d'investigation › Microscopie électronique › Microscopie électronique à balayage › Probing the mechanism of bupivacaine drug...