Development of near zero-order release PLGA-based microspheres of a novel antipsychotic

Zhao, Jinlong; Wang, Lexi; Fan, Chunyu; Liu, Ximing; Zhao, Xiao-Lei; Wang, Dan; Liu, Wenhua; Su, Zhengxing; Sun, Fengying; Li, Youxin

doi:10.1016/j.ijpharm.2016.11.007

Cited by 25 publications

(14 citation statements)

References 28 publications

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“…Hydrophilic medicines often have lower drug loading efficiencies because the drug molecules enter the aqueous phase before the PLGA chains form into particles [ 72 ]. For loading hydrophobic and hydrophilic drugs into PLGA microparticles, the most extensively utilized methods are emulsion-evaporation technique (oil/water or water/oil/water) ( Figure 6 ) [ 73 , 74 , 75 ]. The single emulsion technique involves an organic phase which contains PLGA polymer and the hydrophobic drug in a suitable organic solvent and an aqueous phase which contains a stabilizer.…”

Section: Glass Transition Temperature Of Plga Particlesmentioning

confidence: 99%

Glass Transition Temperature of PLGA Particles and the Influence on Drug Delivery Applications

Liu

McEnnis

2022

Polymers

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Over recent decades, poly(lactic-co-glycolic acid) (PLGA) based nano- and micro- drug delivery vehicles have been rapidly developed since PLGA was approved by the Food and Drug Administration (FDA). Common factors that influence PLGA particle properties have been extensively studied by researchers, such as particle size, polydispersity index (PDI), surface morphology, zeta potential, and drug loading efficiency. These properties have all been found to be key factors for determining the drug release kinetics of the drug delivery particles. For drug delivery applications the drug release behavior is a critical property, and PLGA drug delivery systems are still plagued with the issue of burst release when a large portion of the drug is suddenly released from the particle rather than the controlled release the particles are designed for. Other properties of the particles can play a role in the drug release behavior, such as the glass transition temperature (Tg). The Tg, however, is an underreported property of current PLGA based drug delivery systems. This review summarizes the basic knowledge of the glass transition temperature in PLGA particles, the factors that influence the Tg, the effect of Tg on drug release behavior, and presents the recent awareness of the influence of Tg on drug delivery applications.

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Section: Glass Transition Temperature Of Plga Particlesmentioning

confidence: 99%

Glass Transition Temperature of PLGA Particles and the Influence on Drug Delivery Applications

Liu

McEnnis

2022

Polymers

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“…During the lag phase, an additional prescription (e.g., oral supplementation) may be required, causing inconvenience . A prolonged drug release at a constant rate (zero-order) without any initial burst or delay (monophasic) is currently considered an ideal drug release profile …”

Section: Introductionmentioning

confidence: 99%

Phenomenology of the Initial Burst Release of Drugs from PLGA Microparticles

Yoo

Won

2020

ACS Biomater. Sci. Eng.

225

156

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Poly(lactic-co-glycolic acid) (PLGA) is the most prevalent polymer drug delivery vehicle in use today. There are about 20 commercialized drug products in which PLGA is used as an excipient. In more than half of these formulations, PLGA is used in the form of microparticles (with sizes in the range between 60 nm and 100 μm). The primary role of PLGA is to control the kinetics of drug release toward achieving sustained release of the drug. Unfortunately, most drug-loaded PLGA microparticles exhibit a common drawback: an initial uncontrolled burst of the drug. After 30 years of utilization of PLGA in controlled drug delivery systems, this initial burst drug release still remains an unresolved challenge. In this Review, we present a summary of the proposed mechanisms responsible for this phenomenon and the known factors affecting the burst release process. Also, we discuss examples of recent efforts made to reduce the initial burst release of the drug from PLGA particles.

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“…The zero-order model is usually employed to assume a single-phase ideal condition in which the release kinetics is continuous and can be explained as a function dependent on time and independent of the dissolved concentration in the release medium [ 48 ]. In addition, zero-order behavior can be observed in materials capable of swelling [ 129 ], yet due to complicated bulk erosion and surface erosion and diffusion processes, most studies on the sustained release of hydrophilic drugs have failed to achieve a release profile that conforms to zero-order kinetics for a prolonged time [ 130 ]. This conclusion was verified in this study, in which the data sets had a biphasic behavior far from zero-order according to the low values of R 2 and R 2 a and the high averages of the calculated AIC and BIC [ 131 ].…”

Section: Discussionmentioning

confidence: 99%

Comparative statistical analysis of the release kinetics models for nanoprecipitated drug delivery systems based on poly(lactic-co-glycolic acid)

et al. 2022

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Poly(lactic-co-glycolic acid) is one of the most used polymers for drug delivery systems (DDSs). It shows excellent biocompatibility, biodegradability, and allows spatio-temporal control of the release of a drug by altering its chemistry. In spite of this, few formulations have reached the market. To characterize and optimize the drug release process, mathematical models offer a good alternative as they allow interpreting and predicting experimental findings, saving time and money. However, there is no general model that describes all types of drug release of polymeric DDSs. This study aims to perform a statistical comparison of several mathematical models commonly used in order to find which of them best describes the drug release profile from PLGA particles synthesized by nanoprecipitation method. For this purpose, 40 datasets extracted from scientific articles published since 2016 were collected. Each set was fitted by the models: order zero to fifth order polynomials, Korsmeyer-Peppas, Weibull and Hyperbolic Tangent Function. Some data sets had few observations that do not allow to apply statistic test, thus bootstrap resampling technique was performed. Statistic evidence showed that Hyperbolic Tangent Function model is the one that best fit most of the data.

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Development of near zero-order release PLGA-based microspheres of a novel antipsychotic

Cited by 25 publications

References 28 publications

Glass Transition Temperature of PLGA Particles and the Influence on Drug Delivery Applications

Glass Transition Temperature of PLGA Particles and the Influence on Drug Delivery Applications

Phenomenology of the Initial Burst Release of Drugs from PLGA Microparticles

Comparative statistical analysis of the release kinetics models for nanoprecipitated drug delivery systems based on poly(lactic-co-glycolic acid)

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