The effect of the release behavior of simvastatin from different PLGA particles on bone regeneration in vitro and in vivo : Comparison of simvastatin-loaded PLGA microspheres and nanospheres

Terukina, Takayuki; Naito, Yoshihito; Tagami, Tatsuaki; Morikawa, Yoshinori; Henmi, Yoko; Prananingrum, Widyasri; Ichikawa, Tetsuo; Ozeki, Tetsuya

doi:10.1016/j.jddst.2016.03.005

Cited by 20 publications

(15 citation statements)

References 31 publications

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“…PLGA microspheres providing sustained release of drugs over a wide range of periods can reduce dosing frequency, minimize drug side effects, and improve patient compliance. Emulsion-based solvent evaporation preparative techniques using methylene chloride or chloroform are commonly applied to prepare PLGA particles [1][2][3]. These solvents have low boiling points and negligible water-immiscibility.…”

Section: Introductionmentioning

confidence: 99%

Assessment of Residual Solvent and Drug in PLGA Microspheres by Derivative Thermogravimetry

Shim

Sah

2020

Pharmaceutics

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Thermogravimetry does not give specific information on residual organic solvents in polymeric matrices unless it is hyphenated with the so-called evolved gas analysis. The purpose of this study was to apply, for the first time, derivative thermogravimetry (DTG) to characterize a residual solvent and a drug in poly-d,l-lactide-co-glycolide (PLGA) microspheres. Ethyl formate, an ICH class 3 solvent, was used to encapsulate progesterone into microspheres. DTG provided a distinct peak, displaying the onset and end temperatures at which ethyl formate started to evolve from to where it completely escaped out of the microspheres. DTG also gave the area and height of the solvent peak, as well as the temperature of the highest mass change rate of the microspheres. These derivative parameters allowed for the measurement of the amount of residual ethyl formate in the microspheres. Interestingly, progesterone affected not only the residual solvent amount but also these derivative parameters. Another intriguing finding was that there was a linear relationship between progesterone content and the peak height of ethyl formate. The residual solvent data calculated by DTG were quite comparable to those measured by gas chromatography. In summary, DTG could be an efficient and practical quality control tool to evaluate residual solvents and drugs in various polymeric matrices.

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Section: Introductionmentioning

confidence: 99%

Assessment of Residual Solvent and Drug in PLGA Microspheres by Derivative Thermogravimetry

Shim

Sah

2020

Pharmaceutics

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“…Microsphere size is a primary factor determining drug release rates. 43 In many cases, larger spheres generally release more slowly and over longer time periods, smaller spheres release faster due to increased surface-area-to-volume ratio. Since O-CMCS microspheres had smaller diameters than CS microspheres, the release rate was faster too, and at initial stage, the burst release could be due to the release of protein adhered to the surface of the microspheres.…”

Section: Resultsmentioning

confidence: 99%

“…The medium was changed on alternate days, and the cultures were maintained in an incubator at 37°C in a 5% CO 2 atmosphere. 43…”

Section: Methodsmentioning

confidence: 99%

“…The medium was changed on alternate days, and the cultures were maintained in an incubator at 37°C in a 5% CO 2 atmosphere. 43 Cell proliferation was measured using a WST-8 assay kit (Cell Counting Kit-8 (CCK-8); Dojindo Laboratories, Japan), as per the manufacturer's instruction. MC3T3-E1 were seeded in 24-well plates (8000 cells/well).…”

Section: Cell Culture and Proliferation Assaymentioning

confidence: 99%

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Comparison of chitosan microsphere versus O-carboxymethyl chitosan microsphere for drug delivery systems

Zhou

Zhang

Tai

et al. 2017

Journal of Bioactive and Compatible Polymers

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The development of controlled drug delivery systems for bone regeneration, especially microspheres, has become a research hotspot in recent years. Chitosan and its derivative O-carboxymethyl chitosan have been considered to be an effective way for controlled drug delivery due to their nontoxicity and biodegradability. Currently, most of the studies have researched on synthesizing and characterizing chitosan and O-carboxymethyl chitosan. However, few studies have focused on the differences between chitosan microspheres and O-carboxymethyl chitosan microspheres directly. In this study, chitosan and O-carboxymethyl chitosan microspheres were developed by water-in-oil emulsification cross-linking method using vanillin as the cross-linking agent, and then their physicochemical properties were evaluated by Fourier transform infrared spectroscopy, scanning electron microscopy, and in vitro release testing. The results showed that O-carboxymethyl chitosan was successfully modified by adding carboxymethyl group at the chitosan C6 position.The particle size of chitosan microspheres (50–90 µm) was significantly larger than that of O-carboxymethyl chitosan microspheres (10–50 µm), and the drug release profile of O-carboxymethyl chitosan microspheres showed larger initial burst release within the first day and sustained release at the fourth day, while chitosan microspheres showed sustained release at the seventh day. In addition, Cell Counting Kit-8 assay showed that MC3T3-E1 proliferated well and highly expressed the alkaline phosphatase marker protein on both chitosan and O-carboxymethyl chitosan microspheres. Overall, both chitosan and O-carboxymethyl chitosan microspheres showed good biocompatibility, and chitosan microspheres were superior to O-carboxymethyl chitosan microspheres. Moreover, the different drug release rates suggest that chitosan and O-carboxymethyl chitosan microspheres have the potential to be used for the repair of different bone defects.

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“…Copolymers of lactic acid and glycolic acid (PLGA) as a biodegradable material have been widely used in drug delivery and adjuvant research. 15,16 However, the nal metabolites of the lactic acid and glycolic acid of PLGA may cause subtle changes in the micro-environment in vivo, 17 which results in the decreased stability of the entrapped antigen, or they may become encapsulated in nanoparticles, as well as having a negative impact on the immunogenicity.…”

Section: Introductionmentioning

confidence: 99%

Poly(anhydride) nanoparticles act as effective adjuvants to elicit a persistent immune response

et al. 2017

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The effect of the release behavior of simvastatin from different PLGA particles on bone regeneration in vitro and in vivo : Comparison of simvastatin-loaded PLGA microspheres and nanospheres

Cited by 20 publications

References 31 publications

Assessment of Residual Solvent and Drug in PLGA Microspheres by Derivative Thermogravimetry

Assessment of Residual Solvent and Drug in PLGA Microspheres by Derivative Thermogravimetry

Comparison of chitosan microsphere versus O-carboxymethyl chitosan microsphere for drug delivery systems

Poly(anhydride) nanoparticles act as effective adjuvants to elicit a persistent immune response

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