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Injectable Sustained-Release Depots Of PLGA Microspheres For Insoluble Drugs Prepared By Hot-Melt Extrusion

Yuting Guo, Y. Yang, Luying He, R. Sun, Chenguang Pu, B. Xie, H. He, Y. Zhang, T. Yin, Yanjiao Wang, X. Tang
Published 2017 · Medicine, Chemistry
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PurposeProgesterone (PRG) was selected as a model drug to develop a long-acting injection system for poorly water-soluble drugs.MethodsMicrospheres with high density-low porosity were prepared by hot-melt extrusion (HME) combined with wet-milling as the representative formulation, and a microcrystal suspension was also studied as a comparison. The morphology, particle size and distribution, polymorphism, drug distribution, density and porosity were characterized by scanning electron microscopy, laser diffraction particle size analyzer, power X-ray diffraction and DSC respectively. The in vivo performance of the different formulations within 7 days after intramuscular injection was evaluated in male SD rats.ResultsThe drug-loading rate of the microspheres could be as high as 40%. The average initial burst release of the microspheres (PLGA lactide:glycolide = 75:25) was only 6.7% much lower than that of the microsuspension (25.7%) and a sustained release was exhibited for at least 7 days. The release mechanism was speculated to be as follows. The microspheres are a drug depot with drug microcrystals in the PLGA matrix which is a layer by layer honeycomb structure.ConclusionsMicrospheres prepared by HME combined with wet-milling could achieve a long-term sustained release effect as a novel long-acting formulation strategy.
This paper references
Effectiveness of switching from long-acting injectable fluphenazine or haloperidol decanoate to long-acting injectable risperidone microspheres: an open-label, randomized controlled trial.
N. Covell (2012)
How porosity and size affect the drug release mechanisms from PLGA-based microparticles.
D. Klose (2006)
In situ forming parenteral drug delivery systems: an overview.
C. B. Packhaeuser (2004)
Thermosensitive and pH induced in situ ophthalmic gelling system for ciprofloxacin hydrochloride: hydroxypropyl-beta-cyclodextrin complex.
Berrin Başaran (2012)
Development and Validation of LC-MS/MS Assay for the Quantification of Progesterone in Rat Plasma and its Application to Pharmacokinetic Studies.
Makoto Sasaki (2015)
Subcutaneous or intramuscular? Confronting a parenteral administration dilemma.
Julie Prettyman (2005)
Effect of Experimental Parameters on Alginate/Chitosan Microparticles for BCG Encapsulation
L. A. Caetano (2016)
Nanosuspensions in drug delivery
Barrett E. Rabinow (2004)
Principles of encapsulating hydrophobic drugs in PLA/PLGA microparticles.
C. Wischke (2008)
JW,Williams RO III. Hot-melt extrusion - basic principles and pharmaceutical applications
B Lang (2014)
Enhanced dissolution and oral bioavailability of aripiprazole nanosuspensions prepared by nanoprecipitation/homogenization based on acid-base neutralization.
Y. Xu (2012)
Hot-melt extrusion – basic principles and pharmaceutical applications
B. Lang (2014)
Paliperidone palmitate – review of the efficacy, safety and cost of a new second‐generation depot antipsychotic medication
L. Citrome (2010)
Preparation and characterization of poly(lactic-co-glycolic acid) microspheres loaded with a labile antiparkinson prodrug.
E. D'Aurizio (2011)
In Vitro–In Vivo Characterization of Release Modifying Agents for Parenteral Sustained‐Release Ketorolac Formulation
V. Puri (2004)
Long-acting hormonal contraceptives for women
J. Garza-flores (1991)
CRC Handbook of solubility parameters and other cohesion parameters
A. M. Barton (1983)
Delivery of Soluble Tumor Necrosis Factor Receptor from In-Situ Forming PLGA Implants: In-Vivo
R. Eliaz (2004)
Engineering biodegradable polyester particles with specific drug targeting and drug release properties.
F. Mohamed (2008)
Fundamental understanding of drug absorption from a parenteral oil depot.
R. Kalicharan (2016)
Pharmaceutical Applications of Hot-Melt Extrusion: Part I
Michael M. Crowley (2007)
Using Hansen solubility parameters to study the encapsulation of caffeine in MOFs.
Lorena Paseta (2015)
Polymorphism of Progesterone: A New Approach for the Formation of Form II and the Relative Stabilities of Form I and Form II
Anindita Sarkar (2014)
Pharmaceutical and clinical development of a novel progesterone formulation
Barbara Cometti (2015)
NanoCipro encapsulation in monodisperse large porous PLGA microparticles.
Matthew M Arnold (2007)
Electrospray synthesis and properties of hierarchically structured PLGA TIPS microspheres for use as controlled release technologies.
S. A. Malik (2016)
On the importance and mechanisms of burst release in matrix-controlled drug delivery systems.
X. Huang (2001)
A multivariate approach applied to quality on particle engineering of spray-dried mannitol
T. F. Guimarães (2015)
Poly(lactic-co-glycolic) acid-controlled-release systems: experimental and modeling insights.
D. J. Hines (2013)
Sustained-Release Delivery of Octreotide from Biodegradable Polymeric Microspheres
Yun-Seok Rhee (2011)
Comparative bioavailability study of two haloperidol decanoate containing products
G. V. Weringh (2005)
Development of PLGA-Based Injectable Delivery Systems For Hydrophobic Fenretinide
C. Wischke (2010)
Polymeric topology and composition constrained polyether-polyester micelles for directional antitumor drug delivery.
Di Li (2013)
Injectable Hydrogel-Microsphere Construct with Sequential Degradation for Locally Synergistic Chemotherapy.
Yuhao Zheng (2017)
Strategies for encapsulation of small hydrophilic and amphiphilic drugs in PLGA microspheres: State-of-the-art and challenges.
F. Ramazani (2016)
Tissue distribution and plasma clearance of a novel microcrystal-encapsulated flurbiprofen formulation
MA Clement (1992)
Hydrosols : alternatives for the parenteral application of poorly water soluble drugs
P. Gassmann (1994)
Growth hormone replacement in adults - current standards and new perspectives.
C. Höybye (2015)
LC-MS/MS quantitation of plasma progesterone in cattle.
R.M.T. Fernandes (2011)

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