Antitumor activity of gemcitabine hydrochloride loaded lipid polymer hybrid nanoparticles (LPHNs): In vitro and in vivo

Two-component reduction-sensitive lipid–polymer hybrid nanoparticles composed of DLPE-S-S-MPEG and PCL were developed for intracellular reduction triggered delivery of DOX.

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pH Sensitive Lipid-Polymer Hybrid Nanoparticles Mediated Delivery of Docetaxel: A Viable Approach for Breast Cancer Therapeutic Intervention Development

10.21203/rs.3.rs-23464/v1 ◽

2020 ◽

Author(s):

Ye Yuan ◽

Jia-Xing Song ◽

Mei-Na Zhang ◽

Baoshan Yuan

Keyword(s):

Breast Cancer ◽

Cellular Uptake ◽

Intervention Development ◽

Ph Sensitive ◽

Therapeutic Interventions ◽

Hybrid Nanoparticles ◽

Breast Cancer Cell Lines ◽

Polymer Hybrid

Abstract Present study was planned for the development of pH sensitive lipid polymer hybrid nanoparticles (pHS-LPHNPs) loaded with docetaxel (DTX) for guided and target specific cytosolic-delivery delivery of docetaxel (DTX). pHS-LPHNPs were formulated to entrap DTX by self-assembled nano-precipitation technique and characterised with respect to zeta potential, particle-size, entrapment efficiency, PDI as well as invitro drug release. The cell viability, apoptosis, cellular-uptake, pharmacokinetics, bio-distribution in vital organs, % changes in tumour volume and survival of breast cancer bearing animals were used for the evaluation of efficacy of the formulation. In-vitro studies showed increased cytotoxicity at lower IC50 and better cellular-uptake of pHS-LPHNPs mediated drug by breast cancer cell lines. We saw the better rate of apoptosis of breast cancer cells via Annexin V/Propidium iodide staining. Moreover, in-vivo studies demonstrated improved pharmacokinetics and targetability with minimum drug circulation in deep-seated organs upon delivery of DTX via pHS-LPHNPs in comparison with LPHNPs-DTX and free DTX. We observed sizeable % reduction in tumour-burden with pHS-LPHNPs-DTXthan that withLPHNPs-DTX &free DTX. In brief, pHS-LPHNPs mediated delivery of DTX exhibited promising approach for developing therapeutic-interventions against breast-cancer.

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Codelivery of doxorubicin and triptolide with reduction-sensitive lipid–polymer hybrid nanoparticles for in vitro and in vivo synergistic cancer treatment

International Journal of Nanomedicine ◽

10.2147/ijn.s131235 ◽

2017 ◽

Vol Volume 12 ◽

pp. 1853-1862 ◽

Cited By ~ 25

Author(s):

Bo Wu ◽

Shu-Ting Lu ◽

Liu-Jie Zhang ◽

Ren-Xi Zhuo ◽

Hai-Bo Xu ◽

...

Keyword(s):

Cancer Treatment ◽

Hybrid Nanoparticles ◽

Polymer Hybrid

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Local anesthetic effects of bupivacaine loaded lipid-polymer hybrid nanoparticles: In vitro and in vivo evaluation

Biomedicine & Pharmacotherapy ◽

10.1016/j.biopha.2017.01.175 ◽

2017 ◽

Vol 89 ◽

pp. 689-695 ◽

Cited By ~ 25

Author(s):

Pengju Ma ◽

Ting Li ◽

Huaixin Xing ◽

Suzhen Wang ◽

Yingui Sun ◽

...

Keyword(s):

Local Anesthetic ◽

Hybrid Nanoparticles ◽

In Vivo Evaluation ◽

Polymer Hybrid

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Development of Lipid–Polymer Hybrid Nanoparticles for Improving Oral Absorption of Enoxaparin

Pharmaceutics ◽

10.3390/pharmaceutics12070607 ◽

2020 ◽

Vol 12 (7) ◽

pp. 607

Author(s):

Bo Tang ◽

Yu Qian ◽

Guihua Fang

Keyword(s):

Oral Delivery ◽

Encapsulation Efficiency ◽

Oral Absorption ◽

Poloxamer 407 ◽

Hybrid Nanoparticles ◽

Polymer Hybrid ◽

Study Results ◽

Confocal Scanning

Enoxaparin, an anticoagulant that helps prevent the formation of blood clots, is administered parenterally. Here, we report the development and evaluation of lipid–polymer hybrid nanoparticles (LPHNs) for the oral delivery of enoxaparin. The polymer poloxamer 407 (P407) was incorporated into lipid nanoparticles to form gel cores and ensure high encapsulation efficiency and the controlled release of enoxaparin. In vitro results indicated that 30% of P407 incorporation offered higher encapsulation efficiency and sustained the release of enoxaparin. Laser confocal scanning microscopy (LCSM) images showed that LPHNs could not only significantly improve the accumulation of enoxaparin in intestinal villi but also facilitate enoxaparin transport into the underlayer of intestinal epithelial cells. In vivo pharmacokinetic study results indicated that the oral bioavailability of enoxaparin was markedly increased about 6.8-fold by LPHNs. In addition, its therapeutic efficacy against pulmonary thromboembolism was improved 2.99-fold by LPHNs. Moreover, LPHNs exhibited excellent biocompatibility in the intestine. Overall, the LPHN is a promising delivery carrier to boost the oral absorption of enoxaparin.

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Development of Sustained Release Baricitinib Loaded Lipid-Polymer Hybrid Nanoparticles with Improved Oral Bioavailability

Molecules ◽

10.3390/molecules27010168 ◽

2021 ◽

Vol 27 (1) ◽

pp. 168

Author(s):

Md. Khalid Anwer ◽

Essam A. Ali ◽

Muzaffar Iqbal ◽

Mohammed Muqtader Ahmed ◽

Mohammed F. Aldawsari ◽

...

Keyword(s):

Particle Size ◽

Sustained Release ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Janus Kinase ◽

Hybrid Nanoparticles ◽

Polymer Hybrid ◽

Vitro Release

Baricitinib (BTB) is an orally administered Janus kinase inhibitor, therapeutically used for the treatment of rheumatoid arthritis. Recently it has also been approved for the treatment of COVID-19 infection. In this study, four different BTB-loaded lipids (stearin)-polymer (Poly(d,l-lactide-co-glycolide)) hybrid nanoparticles (B-PLN1 to B-PLN4) were prepared by the single-step nanoprecipitation method. Next, they were characterised in terms of physicochemical properties such as particle size, zeta potential (ζP), polydispersity index (PDI), entrapment efficiency (EE) and drug loading (DL). Based on preliminary evaluation, the B-PLN4 was regarded as the optimised formulation with particle size (272 ± 7.6 nm), PDI (0.225), ζP (−36.5 ± 3.1 mV), %EE (71.6 ± 1.5%) and %DL (2.87 ± 0.42%). This formulation (B-PLN4) was further assessed concerning morphology, in vitro release, and in vivo pharmacokinetic studies in rats. The in vitro release profile exhibited a sustained release pattern well-fitted by the Korsmeyer–Peppas kinetic model (R2 = 0.879). The in vivo pharmacokinetic data showed an enhancement (2.92 times more) in bioavailability in comparison to the normal suspension of pure BTB. These data concluded that the formulated lipid-polymer hybrid nanoparticles could be a promising drug delivery option to enhance the bioavailability of BTB. Overall, this study provides a scientific basis for future studies on the entrapment efficiency of lipid-polymer hybrid systems as promising carriers for overcoming pharmacokinetic limitations.

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Mechanistic profiling of the release kinetics of siRNA from lipidoid-polymer hybrid nanoparticles in vitro and in vivo after pulmonary administration

Journal of Controlled Release ◽

10.1016/j.jconrel.2019.08.004 ◽

2019 ◽

Vol 310 ◽

pp. 82-93 ◽

Cited By ~ 9

Author(s):

Kaushik Thanki ◽

Delphine van Eetvelde ◽

Antonia Geyer ◽

Juan Fraire ◽

Remi Hendrix ◽

...

Keyword(s):

Release Kinetics ◽

Hybrid Nanoparticles ◽

Pulmonary Administration ◽

Polymer Hybrid ◽

Kinetics Of

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Folate-containing reduction-sensitive lipid–polymer hybrid nanoparticles for targeted delivery of doxorubicin

Biomaterials Science ◽

10.1039/c4bm00462k ◽

2015 ◽

Vol 3 (4) ◽

pp. 655-664 ◽

Cited By ~ 33

Author(s):

Bo Wu ◽

Ping Yu ◽

Can Cui ◽

Ming Wu ◽

Yang Zhang ◽

...

Keyword(s):

Drug Delivery ◽

Outer Layer ◽

Targeted Delivery ◽

Hybrid Nanoparticles ◽

Polymer Hybrid

Lipid–polymer hybrid nanoparticles (FLPNPs) containing a folate targeted ligand and a reduction-sensitive outer layer were developed to enhance drug delivery efficacy in vitro and in vivo.

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Non-small cell lung cancer-targeted, redox-sensitive lipid-polymer hybrid nanoparticles for the delivery of a second-generation irreversible epidermal growth factor inhibitor—Afatinib: In vitro and in vivo evaluation

Biomedicine & Pharmacotherapy ◽

10.1016/j.biopha.2019.109493 ◽

2019 ◽

Vol 120 ◽

pp. 109493 ◽

Cited By ~ 6

Author(s):

Jinli Wang ◽

Gaoxing Su ◽

Xiaoqin Yin ◽

Jia Luo ◽

Rongrong Gu ◽

...

Keyword(s):

Small Cell ◽

Hybrid Nanoparticles ◽

Small Cell Lung ◽

In Vivo Evaluation ◽

Polymer Hybrid ◽

Factor Inhibitor ◽

Epidermal Growth Factor Inhibitor ◽

Epidermal Growth

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Norfloxacin Loaded Lipid Polymer Hybrid Nanoparticles for Oral Administration: Fabrication, Characterization, in Silico Modelling and Toxicity Evaluation

Pharmaceutics ◽

10.3390/pharmaceutics13101632 ◽

2021 ◽

Vol 13 (10) ◽

pp. 1632

Author(s):

Muhammad Asghar Khan ◽

Shahzeb Khan ◽

Mohsin Kazi ◽

Sultan M. Alshehri ◽

Muhammad Shahid ◽

...

Keyword(s):

Oral Bioavailability ◽

In Vitro Study ◽

Hybrid Nanoparticles ◽

Process Conditions ◽

Drug Release Profile ◽

Sustained Drug Release ◽

In Vivo Evaluation ◽

Polymer Hybrid

Norfloxacin (NOR), widely employed as an anti-bacterial drug, has poor oral bioavailability. Nano based drug delivery systems are widely used to overcome the existing oral bioavailability challenges. Lipid–Polymer Hybrid Nanoparticles (LPHNs) exhibit the distinctive advantages of both polymeric and liposomes nanoparticles, while excluding some of their disadvantages. In the current study, NOR loaded LPHNs were prepared, and were solid amorphous in nature, followed by in vitro and in vivo evaluation. The optimized process conditions resulted in LPHNs with the acceptable particle size 121.27 nm, Polydispersity Index (PDI) of 0.214 and zeta potential of -32 mv. The addition of a helper lipid, oleic acid, and polymers, ethyl cellulose, substantially increased the encapsulation efficiency (EE%) (65% to 97%). In vitro study showed a sustained drug release profile (75% within 12 h) for NOR LPHNs. The optimized NOR LPHNs showed a significant increase (p < 0.05) in bioavailability compared to the commercial product. From the acute toxicity study, the LD50 value was found to be greater than 1600 mg/kg. The molecular modelling studies substantiated the experimental results with the best combination of polymers and surfactants that produced highly stable LPHNs. Therefore, LPHNs proved to be a promising system for the delivery of NOR, as well as for other antibiotics and hydrophobic drugs.

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