Preparation, Characterization and Related &lt;i&gt;in Vivo&lt;/i&gt; Release, Safety and Toxicity Studies of Long Acting Lanreotide Microspheres

Wang, Shuang; Wu, Mingsheng; Li, Dan; Jiao, Mingli; Wang, Lan; Zhang, Haifeng; Liu, Huai Yu; Wang, Daifeng; Han, Bing

doi:10.1248/bpb.b110726

Cited by 17 publications

(7 citation statements)

References 25 publications

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“…In this study, active systemic anaphylaxis test and passive cutaneous anaphylaxis test were used to evaluate the immunogenicity of prepared microspheres. The following two tests were carried out as Wang et al described with minor modifications [ 31 ].…”

Section: Experiments and Methodsmentioning

confidence: 99%

In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene

Xie

Lin

Xing³

et al. 2015

PLoS ONE

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Poor patient compliance, untoward reactions and unstable blood drug levels after the bolus administration are impeding the pharmacotherapy for insobriety. A long-acting preparation may address these limitations. The aim of this paper was to further investigate the in vitro characteristics and in vivo performances of nalmefene microspheres. Nalmefene was blended with poly (lactide-co-glycolide) (PLGA) to prepare the target microspheres by an O/O emulsification solvent evaporation method. The prepared microspheres exhibited a controlled release profile of nalmefene in vitro over 4 weeks, which was well fitted with a first-order model. In vitro degradation study showed that the drug release in vitro was dominated by both drug diffusion and polymer degradation mechanisms. Pharmacokinetics study indicated that the prepared microspheres could provide a relatively constant of nalmefene plasma concentration for at least one month in rats. The in vivo pharmacokinetics profile was well correlated with the in vitro drug release. Pharmacodynamics studies revealed that the drug loaded microspheres could produce a long-acting antagonism efficacy on rats. These results demonstrated the promising application of injectable PLGA microspheres containing nalmefene for the long-term treatment of alcohol dependence.

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Section: Experiments and Methodsmentioning

confidence: 99%

In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene

Xie

Lin

Xing³

et al. 2015

PLoS ONE

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“…The phosphate buffer at pH 7.4 was used as the in vitro drug release medium of MPEG–PLA–SS–ECA nanoparticles. Five milligrams of nanoparticles were put in a dialysis bag, and then the dialysis bag was placed in a 10 mL PBS medium and vibrated at 37 °C under a constant temperature (80 r/min) for the observation on in vitro release [ 30 , 31 , 32 ]. The samples were taken out at a certain interval, and 10 mL of the release medium were taken out completely and then 10 mL of the fresh medium were supplemented.…”

Section: Methodsmentioning

confidence: 99%

Preparation of GST Inhibitor Nanoparticle Drug Delivery System and Its Reversal Effect on the Multidrug Resistance in Oral Carcinoma

Han

Wang²,

Wang

et al. 2015

Nanomaterials

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During the chemotherapy of cancer, drug resistance is the first issue that chemotherapeutic drugs cannot be effectively used for the treatment of cancers repeatedly for a long term, and the main reason for this is that tumor cell detoxification is mediated by GSH (glutathione) catalyzed by GST (glutathione-S-transferase). In this study, a GST inhibitor, ethacrynic acid (ECA), was designed to be coupled with methoxy poly(ethylene glycol)-poly(lactide) (MPEG–PLA) by disulfide bonds to prepare methoxy poly(ethylene glycol)-poly(lactide)-disulphide bond-mthacrynic acid (MPEG–PLA–SS–ECA) as a carrier material of the nanoparticles. Nanoparticles of pingyangmycin (PYM) and carboplatin (CBP) were prepared, respectively, and their physicochemical properties were investigated. The ECA at the disulfide could be released in the presence of GSH, the pingyangmycin, carboplatin and ECA were all uniformly released, and the nanoparticles could release all the drugs completely within 10 days. The half maximal inhibitory concentration (IC50) of the prepared MPEG–PLA–SS–ECA/CBP and MPEG–PLA–SS–ECA/PYM nanoparticles in drug-resistant oral squamous cell carcinoma cell lines SCC15/CBP and SCC15/PYM cells was 12.68 μg·mL−1 and 12.76 μg·mL−1, respectively; the resistant factor RF of them in the drug-resistant cells were 1.51 and 1.24, respectively, indicating that MPEG–PLA–SS–ECA nanoparticles can reverse the drug resistance of these two drug-resistant cells.

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“…Four 2-month-old rabbits were selected as animal models. 28 In brief, the skin on both sides of the spine was prepared and disinfected with 75% alcohol, 1 mL of PLGA MPs at a concentration of 100 mg/mL was evenly divided into five parts and injected into the left back skin, and the right back skin was injected with an equal volume of CLX-PLGA MPs in the same way. Changes in skin, subcutaneous tissues, and vessels at the injection site were observed visually.…”

Section: Local Skin Irritation Testmentioning

confidence: 99%

Poly(lactic acid-co-glycolic acid)-based celecoxib extended-release microspheres for the local treatment of traumatic heterotopic ossification

Lin

Huang

Wu³

et al. 2022

J Biomater Appl

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Traumatic heterotopic ossification (THO) is a serious and common clinical post-traumatic complication for which there is no effective and safe drug treatment. Routine administration of nonsteroidal anti-inflammatory drugs (NSAIDs) after injury is extensively used approach for THO. However, serious adverse events can occur in the event of an overdose of NSAIDs. In our study, we have developed a poly(lactic acid-co-glycolic acid) (PLGA) microsphere by emulsifying solvent volatilization for the prolonged slow delivery of celecoxib (CLX). Three groups of celecoxib-poly(lactic acid-co-glycolic acid) microspheres (CLX–PLGA MPs) were prepared with particle sizes of 3.75±1.28 μm, 49.56±17.15 μm, and 94.98±42.53 μm. Meanwhile, related parameters of microspheres in each group were studied: drug loading (DL), encapsulation rate (EE), and slow-release behavior. The DL and EE of the 3 CLX–PLGA MPs did not vary significantly, and subsequently, we selected the second drug loading microspheres with a retardation period of about 70 days for subsequent experiments. Moreover, cellular and animal experiments suggest that the microspheres are biocompatible and can be safely applied to localized trauma tissue. Finally, it is demonstrated that CLX–PLGA MPs have an effect on inhibiting the osteogenic differentiation of bone marrow mesenchymal stem cells and have the potential to inhibit ectopic bone formation of the THO model in Sprague-Dawley rat. Therefore, this study suggests that CLX–PLGA MPs are expected to be applied topically in the early post-traumatic period to prevent the development of THO.

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Preparation, Characterization and Related <i>in Vivo</i> Release, Safety and Toxicity Studies of Long Acting Lanreotide Microspheres

Cited by 17 publications

References 25 publications

In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene

In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene

Preparation of GST Inhibitor Nanoparticle Drug Delivery System and Its Reversal Effect on the Multidrug Resistance in Oral Carcinoma

Poly(lactic acid-co-glycolic acid)-based celecoxib extended-release microspheres for the local treatment of traumatic heterotopic ossification

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