Bioavailability enhancement, Caco-2 cells uptake and intestinal transport of orally administered lopinavir-loaded PLGA nanoparticles

Joshi, Garima; Kumar, Arun; Sawant, Krutika

doi:10.1080/10717544.2016.1199605

Cited by 54 publications

(27 citation statements)

References 34 publications

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“…Interestingly, upon brain tumor treatments, different research groups have achieved superior antitumor efficacy by implanting drug-loaded MS directly into the precise and functional brain areas using stereotaxy (Jollivet, 2004 ; Menei et al., 2004 ). Since these studies, the development of polymeric PTX delivery implants with high drug-loading efficiency and sustained drug release is important existing in choosing suitable delivery vehicle (Joshi et al., 2016 ). Poly(lactide-co-glycolide) (PLGA) with excellent biocompatibility and adjustable degradation periods could be ideal as delivery vehicle and the highly hydrophobic PTX could be readily incorporated into hydrophobic PLGA matrices (Ho et al., 2008 ).…”

Section: Introductionmentioning

confidence: 99%

Development of a novel morphological paclitaxel-loaded PLGA microspheres for effective cancer therapy: in vitro and in vivo evaluations

Zhang

Wang

et al. 2018

Drug Delivery

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Sustained release of therapeutic agents into tumor cells is a potential approach to improve therapeutic efficacy, decrease side effects, and the drug administration frequency. Herein, we used the modified double-emulsion solvent evaporation (DSE) method to prepare a novel morphological paclitaxel (PTX) loaded poly(lactide-co-glycolide) (PLGA) microspheres (MS). The prepared rough PTX-PLGA-MS possessed microporous surface and highly porous internal structures, which significantly influenced the drug entrapment and release behaviors. The rough MS with an average particle size of 53.47 ± 2.87 μm achieved high drug loading (15.63%) and encapsulation efficiency (92.82%), and provided a favorable sustained drug release. The in vitro antitumor tests of flow cytometry and fluoroimmunoassay revealed that the rough PTX-PLGA-MS displayed effective anti-gliomas activity and enhanced the cellular PTX uptake through adsorptive endocytosis. Both in vitro and in vivo antitumor results demonstrated that the sustained-release PTX could induce the microtubules assembly and the over-expression of Bax and Cyclin B1 proteins, resulting in the microtubule dynamics disruption, G2/M phase arrest, and cell apoptosis accordingly. Furthermore, as the rough PTX-PLGA-MS could disperse and adhere throughout the tumor sites and cause extensive tumor cell apoptosis with one therapeutic course (12 days), they could reduce the system toxicity and drug administration frequency, thus achieving significant tumor inhibitory effects with rapid sustained drug release. In conclusion, our results verified that the rough PTX-PLGA-MS drug release system could serve as a promising treatment to malignant glioma.

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Section: Introductionmentioning

confidence: 99%

Development of a novel morphological paclitaxel-loaded PLGA microspheres for effective cancer therapy: in vitro and in vivo evaluations

Zhang

Wang

et al. 2018

Drug Delivery

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“…With the goal of overcoming the challenge of CuB’s poor solubility and permeability, the present study aimed to investigate a novel mixed micelles modified by CPs. Mixed micelles system could be used to improve the unfavorable solubility and bioavailability of hydrophobic drugs (Joshi et al., 2016 ; Zhang et al., 2017 ). The mixed nanomicelles in the paper composed of Labrasol and Kolliphor HS 15 not only could improve the solubility of CuB, but also negatively charged.…”

Section: Introductionmentioning

confidence: 99%

Modified mixed nanomicelles with collagen peptides enhanced oral absorption of Cucurbitacin B: preparation and evaluation

Tang

Zhu

et al. 2018

Drug Delivery

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Polymer nanoparticles modified with collagen peptides (CPs) are an attractive strategy for the oral delivery of active ingredients from Chinese medicine. Thus, in the present study, collagen cationic CPs were simply separated using ion-exchange resin from bovine CPs, to modify mixed nanomicelles (MMs) on the surface to improve the oral bioavailability of Cucurbitacin B (CuB). The physicochemical property of micelles was characterized, which confirmed the successful modification of the nanomicelles. CPs-modified nanomicelles in vitro were found to significantly increase cellular uptake and transportation. Compared to unmodified micelles, the quantity of CPs-modified micelles internalized by Caco-2 cells were 3.74 times greater and the cumulative transportation flux (AP-BL) was 2.81 times greater. The membrane transportation process of CuB-MMs-CPs was found to be associated with energy consumption and clathrin- and caveolin-mediated endocytosis. In vivo studies performed on rats indicated that in comparison to CuB and CuB-MMs, the relative bioavailability of CuB-MMs-CPs increased by 3.43 times and 2.14 times, respectively. In addition, the tumor inhibition caused by CuB-MMs-CPs was increased significantly. Therefore, the nanomicelles co-modified with isolated CPs could act as attractive carriers for oral delivery of CuB.

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“…Thus, bypassing transporters and CYP3A4 is considered as an effective strategy to improve the ART drug intracellular concentrations, especially in monocytic cells. Literatures suggest that nanoparticles-based drug delivery would bypass the efflux transporters namely P-gp [37] , as well as CYP-mediated liver metabolism [38] . Based on our findings we hypothesize that higher concentration of EVG in PLGA-EVG than EVG alone results from its likely protection from drug transporter P-gp and metabolic enzyme CYP3A4 ( Fig.…”

Section: Discussionmentioning

confidence: 99%

Novel elvitegravir nanoformulation approach to suppress the viral load in HIV-infected macrophages

Gong

Chowdhury

Midde

et al. 2017

Biochemistry and Biophysics Reports

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PurposeMonocytes serve as sanctuary sites for HIV-1 from which virus is difficult to be eliminated. Therefore, an effective viral suppression in monocytes is critical for effective antiretroviral therapy (ART). This study focuses on a new strategy using nanoformulation to optimize the efficacy of ART drugs in HIV-infected monocytes.MethodsPoly(lactic-co-glycolic acid) (PLGA)-based elvitegravir nanoparticles (PLGA-EVG) were prepared by nano-precipitation technique. The physicochemical properties of PLGA-EVG were characterized using transmission electron microscopy, dynamic light scattering, and Fourier-transform infrared spectroscopy. Cellular uptake study was performed by fluorescence microscopy and flow cytometry. All in vitro experiments were performed by using HIV-infected monocytic cell lines U1 and HIV-infected primary macrophages. Elvitegravir quantification was performed using LC-MS/MS. HIV viral replication was assessed by using p24 ELISA.ResultsWe developed a PLGA-EVG nanoparticle formulation with particle size of ~ 47 nm from transmission electron microscopy and zeta potential of ~ 6.74 mV from dynamic light scattering. These nanoparticles demonstrated a time- and concentration-dependent uptakes in monocytes. PLGA-EVG formulation showed a ~ 2 times higher intracellular internalization of EVG than control group (EVG alone). PLGA-EVG nanoparticles also demonstrated superior viral suppression over control for a prolonged period of time.ConclusionsPLGA-based EVG nanoformulation increased the intracellular uptake of EVG, as well as enhanced viral suppression in HIV-infected macrophages, suggesting its potential for improved HIV treatment in monocytic cells.

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Bioavailability enhancement, Caco-2 cells uptake and intestinal transport of orally administered lopinavir-loaded PLGA nanoparticles

Cited by 54 publications

References 34 publications

Development of a novel morphological paclitaxel-loaded PLGA microspheres for effective cancer therapy: in vitro and in vivo evaluations

Development of a novel morphological paclitaxel-loaded PLGA microspheres for effective cancer therapy: in vitro and in vivo evaluations

Modified mixed nanomicelles with collagen peptides enhanced oral absorption of Cucurbitacin B: preparation and evaluation

Novel elvitegravir nanoformulation approach to suppress the viral load in HIV-infected macrophages

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