Poly(ethylene carbonate)-containing polylactic acid microparticles with rifampicin improve drug delivery to macrophages

Priemel, Petra A.; Wang, Yingya; Bohr, Adam; Water, Jorrit J.; Yang, Mingshi; Nielsen, Hanne Mørck

doi:10.1111/jphp.12937

Cited by 11 publications

(3 citation statements)

References 44 publications

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“…Because of the high content of polylactic acid in copolymer, RIF is encapsulated in micelles. And due to hydrophobic interaction, it is easily loaded into the hydrophobic core, with high drug solubility [ 20 , 21 ]. Previous research [ 22 ] has shown that the formation of HPMA-PLA-RIF copolymer micelles enhanced the efficacy of drugs, improved the solubility of drugs, and combated the resistance of tuberculostatics.…”

Section: Discussionmentioning

confidence: 99%

Protective Effect of Rifampicin Loaded by HPMA-PLA Nanopolymer on Macrophages Infected with Mycobacterium Tuberculosis

Wang

Liu

et al. 2022

Computational and Mathematical Methods in Medicine

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Purpose. This research was designed to investigate the protective effect of rifampicin (RIF) loaded by N-(2-hydroxypropyl) methylacrylamide- (HPMA-) polylactic acid (PLA) nanopolymer on macrophages infected with Mycobacterium tuberculosis (MTB). Methods. We first induced H37Rv to infect macrophages to build a cell model. Then, the HPMA-PLA nanopolymer loaded with RIF was prepared to treat MTB-infected macrophages. The macrophage activity was tested by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, the nitric oxide (NO) in cells was measured through Griess reagent, and the bacterial activity of MTB was observed via the colony-forming unit (CFU) assay. The inflammation-related factors in cells were detected via the enzyme-linked immunosorbent assay (ELISA), the apoptosis of macrophages was examined via flow cytometry, and the expression of apoptosis-related proteins was determined by western blot (WB). Results. HPMA-PLA had no obvious toxicity to macrophages. The expression of NO and inflammatory factors in macrophages infected with MTB increased significantly, but the apoptosis rate was not significantly different from that of uninfected cells. However, after treatment with HPMA-PLA-RIF or free RIF, the inflammatory reaction of infected cells was inhibited, the expression of NO was decreased, the apoptosis rate was increased, and the bacterial activity in cells was decreased, with statistically significant differences; moreover, HPMA-PLA-RIF was more effective than free RIF. Conclusions. HPMA-PLA-RIF has a high protective effect on macrophages infected with MTB, with high safety. Its protective mechanism is at least partly through inhibiting the production of NO and inflammatory response, which can inhibit bacterial activity and induce cell apoptosis.

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Section: Discussionmentioning

confidence: 99%

Protective Effect of Rifampicin Loaded by HPMA-PLA Nanopolymer on Macrophages Infected with Mycobacterium Tuberculosis

Wang

Liu

et al. 2022

Computational and Mathematical Methods in Medicine

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“…In particular, polyesters based therapeutics gain success in improving chemotherapeutic efficacy, both in vitro and in vivo, and anti-inflammatory response for treatment of cancer (Hu and Zhang 2012) and inflammatory diseases (Danhier et al 2012) respectively in various administration routes. Bioinert and biodegradable PLA and PLGA drug carrier materials hold outstanding advantages, including (i) sustainable delivery (Mansor et al 2018), (ii) proper control of drug release kinetics (iii) diminished fluctuations of blood drug concentrations (Makadia and Siegel 2011), (iv) augmented cellular uptake of NPs via endocytosis (Bi et al 2016;Priemel et al 2018), (v) enhanced stability (Xiong et al 2016), (vi) optimal clinical utility (Lü et al 2009) and (vii) improved medication adherence (Liu et al 2006).…”

Section: Pla and Plga Based Mps And Nps Systems For Drug Deliverymentioning

confidence: 99%

Biocompatibility, biodegradation and biomedical applications of poly(lactic acid)/poly(lactic-co-glycolic acid) micro and nanoparticles

Elmowafy

Tiboni

Soliman

2019

J. Pharm. Investig.

390

208

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Background Poly(lactic acid) (PLA) and poly(lactic-co-glycolic acid) (PLGA) are among the well-documented FDAapproved polymers used for the preparation of safe and effective vaccine, drug and gene delivery systems using well-described reproducible methods of fabrication. Various nano and microparticulates are fabricated using these polymers. Their successful performance relies on PLA and PLGA biocompatibility and degradability characteristics. Area covered This review provides an overview of the biocompatibility and biodegradation of PLA, PLGA and their copolymers, with a special emphasis on tissue responses for these polymers as well as their degradation pathways and drug release models. Moreover, the potential of PLA and PLGA based nano and microparticulates in various advanced biomedical applications is highlighted. Expert opinion PLA and PLGA based delivery systems show promises of releasing different drugs, proteins and nucleic acids in a stable and controlled manner and greatly ameliorating their therapeutic efficacy. In addition, advancement in surface modification and targeting of nanoparticles has extended the scope of their utility.

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“…Substantial research has been done to develop alveolar macrophage targeting for pulmonary delivery wherein the drugs are entrapped in polymers, copolymers and lipids. Such formulations include microparticles [6][7][8] , nanoparticles 5,9 , solid lipid nanoparticles 2 etc.…”

Section: Introductionmentioning

confidence: 99%

Therapeutic Management of Pulmonary Tuberculosis by Mannosylated Chitosan Ascorbate Microspheres: Preparation and Characterization

Bagre

Lariya

Kori

2019

J. Drug Delivery Ther.

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Objective: In this study, biodegradable Chitosan Ascorbate Microsphere (CAMs) and mannosylated chitosan ascorbate microsphere (m-CAMs) prepared for targeting towards alveolar macrophages to treatment of pulmonary tuberculosis. Significance: Ascorbic acid is an antioxidant and reported killing effect on mycobacterium by induces fenton reaction. This study enlightens the possible benefits of adding antioxidant properties of ascorbic acid with chitosan microsphere to an anti-tuberculosis regimen and mannosylation of microsphere significantly induce the targetability of antitubercular drug to alveolar macrophages. Methods: CAMs prepared by firstly salification of chitosan by ascorbic acid then ionic gelation with STPP and m-CAMs prepared by incubation method and purified for further studies. The physicochemical, in vitro and in vivo characterizations of both formulations were carried out. Results: The size of microspheres (both CAMs and m-CAMs) were found to be in range of 3.40-4.81µm. Evident changes were observed in crystallinity and structure of both carrier systems and depicted by Fourier transform infrared (FTIR), Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) studies. In vitro lung deposition study of microspheres showed favourable aerodynamic properties for deep lung delivery (MMAD 2.0- 3.8 μm) and, thus, show potential for an application as inhalable tuberculosis therapy. The drug release showed the biphasic pattern of release, i.e., initial burst (30-45% up to 8 h) followed by a slower sustained release pattern (more than 80% up to 72 h) in both simulated lung fluids. Optimized formulations exhibited lower cytotoxicity and bio distribution studies demonstrated the efficiency of m-CAMs for spatial delivery of INH to alveolar tissues. CAMs and m-CAMs evidenced minor cytotoxicity on lung epithelial cells (A549 cell lines). Conclusion: m-CAMs thus has a promising potential to be explore as an effective carrier system for delivery of antitubercular drugs regimen. Key words: Targetability, alveolar macrophage, lung cancer A549 cells

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Poly(ethylene carbonate)-containing polylactic acid microparticles with rifampicin improve drug delivery to macrophages

Abstract: The inclusion of PEC in PLA microparticles increased the release of RF and the inhibitory effect against two bacteria species while displaying physical particle properties similar to PLA particles.

Cited by 11 publications

References 44 publications

Protective Effect of Rifampicin Loaded by HPMA-PLA Nanopolymer on Macrophages Infected with Mycobacterium Tuberculosis

Protective Effect of Rifampicin Loaded by HPMA-PLA Nanopolymer on Macrophages Infected with Mycobacterium Tuberculosis

Biocompatibility, biodegradation and biomedical applications of poly(lactic acid)/poly(lactic-co-glycolic acid) micro and nanoparticles

Therapeutic Management of Pulmonary Tuberculosis by Mannosylated Chitosan Ascorbate Microspheres: Preparation and Characterization

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