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Chinese materia medica has a wide range of clinical applications， but it has many active ingredients with different physicochemical properties， and the target organs， action pathways and mechanisms for different ingredients to exert their efficacy are not the same. Therefore， it is difficult to design and develop a co-delivery system loading multiple components of Chinese materia medica to maximize the synergistic therapeutic efficiency. Based on the characteristics of effectiveness and functionality of active ingredients， the strategies for multi-component co-delivery of Chinese materia medica can be categorized into two types：firstly， based on the effectiveness of active ingredients， new carriers such as liposomes， nanoparticles can be constructed to load multi-components of Chinese materia medica. secondly， based on the functionality of some active ingredients of Chinese materia medica， they are employed in the construction of co-delivery system， which can give play to the dual characteristics of their own efficacy and preparation functions. In this paper， we summarized the relevant research progress of the above two types of multi-component co-delivery strategies， and mainly discussed the pharmaceutical functions of the active ingredients in co-delivery systems， in order to find a more suitable multi-component co-delivery strategy， promoting the design and development of new delivery systems of Chinese materia medica.
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Pulmonary hypertension (PH) is an insidious pulmonary vasculopathy with high mortality and morbidity and its underlying pathogenesis is still poorly delineated. The hyperproliferation and apoptosis resistance of pulmonary artery smooth muscle cells (PASMCs) contributes to pulmonary vascular remodeling in pulmonary hypertension, which is closely linked to the downregulation of fork-head box transcriptional factor O1 (FoxO1) and apoptotic protein caspase 3 (Cas-3). Here, PA-targeted co-delivery of a FoxO1 stimulus (paclitaxel, PTX) and Cas-3 was exploited to alleviate monocrotaline-induced pulmonary hypertension. The co-delivery system is prepared by loading the active protein on paclitaxel-crystal nanoparticles, followed by a glucuronic acid coating to target the glucose transporter-1 on the PASMCs. The co-loaded system (170 nm) circulates in the blood over time, accumulates in the lung, effectively targets the PAs, and profoundly regresses the remodeling of pulmonary arteries and improves hemodynamics, leading to a decrease in pulmonary arterial pressure and Fulton's index. Our mechanistic studies suggest that the targeted co-delivery system alleviates experimental pulmonary hypertension primarily via the regression of PASMC proliferation by inhibiting cell cycle progression and promoting apoptosis. Taken together, this targeted co-delivery approach offers a promising avenue to target PAs and cure the intractable vasculopathy in pulmonary hypertension.
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In recent years, the use of active substances as excipients or as substitutes for other excipients in the design of modern drug delivery systems has received widespread attention, which has promoted the development of the theory of unification of medicines and excipients in the design of traditional Chinese medicine(TCM) preparations. Adopting the theory of unification of medicines and excipients to design drug delivery systems can reduce the use of excipients and thus the cost of preparations, reduce drug toxicity, increase drug solubility and biocompatibility, enhance synergistic effect, and realize targeted delivery and simultaneous delivery of multiple components. However, the research on the application of this theory in the modern drug delivery system of TCM preparations is still insufficient, with few relevant articles. In addition, the TCM active substances that can be used as the excipients remain to be catalogued. In this paper, we review the types and applications of the drug delivery systems with TCM active substances as excipients and describe their common construction methods and mechanisms, aiming to provide references for the in-depth research on the modern drug delivery systems for TCM preparations.
Subject(s)
Medicine, Chinese Traditional , Excipients , Drugs, Chinese Herbal , Nanomedicine , Pharmaceutical PreparationsABSTRACT
Breast cancer is the malignancy with the highest number of new cases worldwide and is the leading cause of cancer-related deaths in women. More than 90% of breast cancer-related deaths are related to its metastasis. Paclitaxel, one of the most commonly used chemotherapeutic agents for the treatment of breast cancer, is an effective means of inhibiting breast cancer metastasis. To overcome the adverse effects of paclitaxel's hydrophobicity and its co-solvent, its nano-drugs have been a hot research topic. Some nanomedicines delivering paclitaxel have been used in clinical practice and have shown satisfactory efficacy and good tolerability. In this review, the research progress on the inhibition of breast cancer metastasis by co-delivered paclitaxel nanomedicines was summarized with the aim of providing a reference for their anti-breast cancer metastasis research.
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Objective @#To fabricate a co-delivery system of curcumin (CUR) and siRNA based on mesoporous silica nanoparticles (MSN) and investigate its potential application in inducing macrophage M2 polarization.@*Methods@# MSNs were synthesized using the conventional sol-gel method. The interior mesochannels were occupied by small-molecule CUR, while the exterior surface was adsorbed by cationic polymeric polyethyleneimine (PEI) to link the negatively charged siRNA molecules to formulate the (CUR@MSN)PEI/siRNA co-delivery system. The formulation process was monitored by transmission electron microscopy(TEM). The MTT assay was used to evaluate the cytotoxicity in RAW264.7 cells under various concentrations of nanoparticles. Confocal laser scanning microscopy and TEM were used to observe cell internalization using FAM-labeled siRNA. GAPDH-targeting siRNA was used to prepare nanoparticles and then was transfected into RAW264.7 cells to observe the silencing efficiency of target genes. The knockdown efficiency was examined by real-time quantitative PCR. The related control groups were untreated cells, CUR delivery only and the co-delivery of CUR and siRNA negative control. By loading miRNA-130a-3p antisense oligonucleotide (ASO) to transfect RAW264.7 cells, the effects on the polarization of macrophages were observed. The M2 polarization marker arginase 1 (Arg-1) was measured by western blotting. The related control groups were untreated cells, CUR delivery only and co-delivery of CUR and miRNA negative control. @* Results @# The (CUR@MSN)PEI/siRNA co-delivery system was successfully formulated. The nanoparticles exhibited dose-dependent cytotoxicity, and the cell viability was maintained over 90% when the nanoparticle concentration was less than 10 μg/mL. A high cell uptake efficiency was observed, and the target gene knockdown efficiency was greater than 80% (P < 0.05 vs. all the other groups). The CUR delivery-only group and co-delivery of the CUR-and miRNA-negative control group improved Arg-1 expression ~ 3-fold (P < 0.05 vs. untreated cells). Using the co-delivery of CUR and ASO, synergistic effects were obtained, and Arg-1 expression was increased ~ 8-fold (P < 0.05 vs. all the other groups).@*Conclusion @#The CUR-siRNA co-delivery system can effectively transfect macrophages and synergistically induce M2 polarization.
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Co-delivery of chemotherapeutics and immunostimulant or chemoimmunotherapy is an emerging strategy in cancer therapy. The precise control of the targeting and release of agents is critical in this methodology. This article proposes the asynchronous release of the chemotherapeutic agents and immunostimulants to realize the synergistic effect between chemotherapy and immunotherapy. To obtain a proof-of-concept, a co-delivery system was prepared
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Objective: To prepare the cationic solid lipid nanoparticles (Que/mR150 SLNs) co-loaded with quercetin (Que) and microRNA-150 (mR150) and investigate the preparation process, then assess its in vitro release, cell uptake capacity and safety of ocular administration. Method: First, thin-film dispersion method was used to prepare quercetin-encapsulated cationic solid lipid nanoparticles (Que-SLNs), and the preparation process was optimized based on the particle size, PDI and encapsulation rate; Using electrostatic adsorption method to co-load mR150 in nanoparticles (Que/mR150 SLNs), and the adsorption efficiency of the miRNA by the nanoparticles was examined by agarose gel electrophoresis experiment; The in vitro release performance of quercetin in Que/mR150 SLNs was investigated; The effect of Que/mR150 SLNs on the proliferation of HUVEC of human umbilical vein endothelial cells was measured by MTT method, and fluorescence labeling was used to observe their uptake in HUVEC; And the irritancy of Que/mR150 SLNs to rabbit eyes was examined by pathological tissue sections of rabbit eyes. Result: After process optimization, the cationic nano Que-SLNs had good drug-loading, particle size distribution and stability. The appearance of the cationic nano-Que-SLNs was spherical, and it could be kept stable for two months. The quercetin encapsulation rate was (85.25 ± 1.29)%, the drug load was (1.67 ± 0.02)%, the average particle size was (110.00 ± 2.10) nm, and the Zeta potential is (53.2 ± 5.12) mV; The in vitro drug release results showed that the release of quercetin in the nanoparticles was slow, and the cumulative release amount within 48 h was about (80.69 ± 1.29)%; When the mass ratio of dioctadecyl dimethyl ammonium bromide to mR150 (DDAB/RNA) of different cationic materials was 6:1, the cationic solid lipid nanoparticles basically encapsulated mR150 completely with little effect on its particle size and potential. MTT experiments showed that blank nanometer mass concentration of 50-150 mg/L had no significant proliferation toxicity on HUVEC cells; Cell uptake experiments showed that Cy5 and coumarin-6 dual fluorescently labeled and co-loaded nanometers could effectively enter HUVEC cells; Pathological tissues of rabbit eyes showed that Que/mR150 SLNs had no obvious damage to the eyes. Conclusion: The preparation process of Que/mR150 SLNs solid lipid nanoparticles is stable and reliable, with good reproducibility, storage stability and good biological safety, which is conducive to the efficient delivery of quercetin and mR150 into HUVEC cells, which provides the ideas for the treatment of diseases related to angiogenesis
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In recent years, multi-modal combined anti-tumor has become an effective strategy for clinical tumor treatment. Photothermal therapy with its characteristics of minimally invasive, controllable, high efficiency, and strong specificity, can effectively make up for the toxic side effects and tumor resistance caused by traditional drug treatment. The research shows that the combination of photothermal therapy and chemotherapy has better synergistic antitumor effect. However, chemotherapeutic drugs and photothermal agents may have different pharmacokinetic behaviors in vivo, so it is difficult to ensure their effective transmission in tumor site, and the free form is easy to be metabolized and degraded in vivo. How to deliver the two therapeutic modes of drugs / photothermal reagents to tumor tissues in a specific, efficient and synchronous manner to achieve the best combined antitumor effect is an important problem to be solved in the combined antitumor application. The development of nano-drug delivery technology provides a new idea for the application of tumor treatment. In this paper, combined with the latest research progress in this field, the anti-tumor mechanism of photothermal therapy combined with chemotherapy, the advantages of nano drug delivery, the types and characteristics of commonly used nano materials and the principle of drug delivery are reviewed in order to provide a reference for the further development of multi-mode combined treatment of tumor.
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OBJECTIVE: To prepare siRNA/HDL modified Dox/micelle multimeric polymer(siRNA/HDL-Dox/micelle) by using HDL as a siRNA carrier and a targeting ligand and to realize the effective co-delivery of siRNA and antitumor drug. METHODS: HDL was incubated with chol-siRNA to prepare siRNA/LDL complex, then coupled with Dox/micelle to form siRNA/HDL modified Dox/micelle multimeric polymer (siRNA/HDL-Dox/micelle). The particle size and stability were investigated in different medium. HepG2/ADM with P-glycoprotein(P-gp) over-expressed were used to study the cell uptake, sub-cellular localization and anti-tumor efficacy in vitro. The ability of siRNA to silence target genes at mRNA and protein level was examined by RT-PCR and Western blot. RESULTS: HDL exhibited an efficient binding ability for siRNA and protected siRNA from RNase. The size and surface morphology of siRNA/HDL-Dox/micelle confirmed by TEM showed that most of the micelles were compact and spherical, exhibited a narrow size distribution and good dispersion. The particle size and Zeta potential increased with increasing incubation time in pH 5.3 PBS. The siRNA was efficiently delivered into the cells by encapsulation into HDL, and the expression of P-gp is effectively down-regulated at the mRNA level and the protein level, thereby increasing the accumulation of intracellular Dox and enhancing the antitumor activity. CONCLUSION: siRNA/HDL-Dox/micelle could effectively deliver siRNA and Dox into tumor cells, thereby exerting gene silencing, reversing tumor drug resistance and enhancing anti-tumor effect.
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OBJECTIVE: To prepare a reduction-responsive nanoparticle (HID-NPs) for indomethacin (IND) and doxorubicin (DOX) delivering and investigate their effects on reversing multidrug resistance in breast cancer. METHODS: Hyaluronic acid-based amphiphilic substances (HA-SS-PA) were prepared by amidation reaction, and their structures were confirmed by NMR. HID-NPs were prepared by nano-precipitation method. The particle size measurement and morphology observation of the HID-NPs were measured by dynamic light scanning (DLS) and transmission electron microscopy (TEM), respectively. The reduction-responsive drug release behavior of HID-NPs was determined by dialysis method. Cell uptake HID-NPs on human breast cancer MCF-7/ADR cells were observed by laser confocal microscopy. The cytotoxicity of HID-NPs on human breast cancer MCF-7 and MCF-7/ADR cells was determined by MTT assay. RESULTS: 1H-NMR spectrum indicated that HA-SS-PA was successfully prepared. The results of DLS and TEM showed that HID-NPs were round and evenly distributed with an average particle size of (103±3.2) nm. Drug release assay indicates that HID-NPs have good reduction-responsiveness ability. Cell uptake experiments demonstrated that HID-NPs significantly increased DOX accumulation in MCF-7/ADR cells compared with free DOX; MTT assays showed that HID-NPs could significantly destroy MCF-7/ADR cells. CONCLUSION: HID-NPs shows good reduction-responsiveness and obvious reverse DOX resistance, which can be used for the treatment of multidrug resistance of breast tumors.
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Anti-tumor intervention using a combination of drugs shows unique advantages in research and clinical practice. Active ingredients of Chinese herbal medicines can offer many advantages, such as high efficiency, low toxicity, wide effect and multiple targets. At present, the combination active ingredients of Chinese herbal and chemotherapy drugs have attracted increased attention. Nano-drug delivery system provides a good carrier platform for anti-tumor drugs. Nano-carrier-mediated drug combination is a promising strategy. In this paper, we review the mechanisms of the anti-tumor effects of active ingredients of traditional Chinese medicine combined with chemotherapeutic drugs and consider the advantages of drug-loaded nanoparticles, the types and characteristics of carriers. The aim is to provide a reference for the research of effective regimen for anti-tumor therapy.
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Objective To study the maturation and activation effects of hyaluronic acid (HA) modified polymer nanoparticles co-delivering adjuvants and antigens on mouse bone marrow dendritic cells (BMDCs). Methods HA-modified polylactic acid-glycolic acid copolymer (PLGA) and cationic lipid DOTAP were used as nanocarriers (DOTAP-PLGA) to co-deliver adjuvant CpG with model antigen ovalbumin (OVA). In the drug-loaded nanocarriers, CpG was covalently bound to the surface of HA, and OVA was physically blended into DOTAP-PLGA nanocarriers. The nanoparticles were characterized by transmission electron microscopy and dynamic light scattering. The in vitro release of CpG and OVA in the nanoparticles was investigated. The uptake and distribution of nanoparticles in mouse BMDCs were studied by flow cytometry and laser scanning confocal microscopy. The maturation and cytokine expression of mouse BMDCs were evaluated by flow cytometry and enzyme-linked immunosorbent assay, respectively. Results The CpG-HA-OVA-PLGA nanoparticles loading CpG and OVA were prepared. The average particle size was (305.1±2.2) nm and the polydispersity index was 0.203. A core-shell structure of the nanoparticles modified by HA was clearly observed by transmission electron microscopy. Cellular experiment results showed that CpG-HA-OVA-PLGA nanoparticles could be efficiently uptaken by mouse BMDCs, and promote lysosomal release of CpG and cytoplasmic delivery of antigen OVA. Compared with free OVA group and free OVA+CpG group, the CpG-HA-OVA-PLGA nanoparticles significantly up-regulated the expression of co-stimulatory molecules CD86 and CD40 (all P<0.01), major histocompatibility complex I (MHC-I) (P<0.01), and cytokine tumor necrosis factor-α (TNF-α) (P<0.01). Conclusions HA-modified CpG and OVA nanoparticle co-delivery vectors can effectively promote the maturation and activation of dendritic cells, which provides a basis for the development of novel vaccine vectors for the co-delivery of antigens and adjuvants.
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Objective To prepare a lipoic acid (LA) modified intrinsically disordered protein-cytosol-localizing internalization peptide 6 (CL) nanocomplex (LA-CL) entering cells by non-endocytosis mechanism for co-delivery of gene and chemotherapeutic drugs, and to investigate its transfection efficiency and cellular uptake on human embryonic kidney cell line HEK293 cells and its release behavior in vitro. Methods We synthesized four disulfide cross-linked lipoic acid modified LA-CLss(1-4) at different cross-linked degrees using different mass fractions (2.5%, 5%, 10% and 20%) of cysteine as cross-linking agent. The construction of LA-CLss was characterized by1H nuclear magnetic resonance (1HNMR) and gel permeation chromatography. The LA-CLss/plasmid enhanced green fluorescent protein (pEGFP) nanocomplexes were self-assembled with LA-CLss and pEGFP at different nitrogen/phosphorus (N/P) ratios (2.5, 5, 10, 20, 40 and 80). The size and zeta potential of LA-CLss/pEGFP nanocomplexes were determined by particle size analyzer, and the pEGFP enrichment capacity of LA-CLss was determined by agarose gel electrophoresis. The docetaxel (DTX)-loaded micelles were prepared by ultrasonic emulsification, and the critical micelle concentration of LA-CLss3 was determined by pyrene fluorescence probe spectroscopy. The LA-CLss/pEGFP nanocomplexes were co-cultured with HEK293 cells, and the transfection efficiencies of LA-CLss/pEGFP nanocomplexes at different cross-linked degrees were investigated. Results1 HNMR results showed the LA-CLss was successfully synthesized. When N/P ratio was 40, the transfection efficiency of LA-CLss3/pEGFP nanocomplex by HEK293 cells was significantly higher than that of LA-CL/pEGFP, LA-CLss1/pEGFP, LA-CLss2/pEGFP and LA-CLss4 nanocomplexes. The encapsulation efficiency and drug loading of docetaxel-loaded micelles prepared by ultrasonic emulsification were (85.25±0.04)% and (8.81±0.02)%, respectively. Cellular uptake test showed that the gene could be effectively delivered into the HEK293 cells by the LA-CLss micelles. In vitro release experiments showed that the LA-CLss micelles had redox-responsive drug release behavior. Conclusion The prepared LA-CLss/DTX/pEGFP nanocomplex is expected to become an efficient vector for co-delivery of gene and chemotherapeutic drugs.
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The efficacy of antineoplastic drugs in cancer treatment is often hampered by drug resistance of tumor cells, which is usually caused by abnormal gene expression. The formation mechanism of multidrug resistance is very complex. Conventional drugs or gene therapy usually only aim at a specific drug target, so it is difficult to effectively control the complex signaling pathways of drug-resistant cells. The co-delivery of small RNA (siRNA ormiRNA) and anti-tumor drugs with nanocarriers can maximize the synergistic effect, and reverse the multidrug resistance of tumor cells by silencing some related proteins. This review summarizes the mechanisms and advantages of the combination therapies involving RNA and antineoplastic drugs, in vitro and in vivo evaluation, as well as the recent advances in the co-delivery nanocarriers for these agents.
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With the development of polymeric materials and nanotechnology, the potential application of nanoscaled drug delivery system (NDDS) is gradually manifested in the field of pharmaceutics. Especially, NDDS has the obvious advantages in the delivery of gene or drug. Comparing to the delivery system of single-drug, co-delivery system of gene and drug can significantly improve the therapeutic effects by enhancing transfection efficiency of gene and reversing multidrug resistance, etc. The co-delivery systems of gene and drug, which had the triggered release characteristics in the inner and outer of tumor, could be constructed by introducing the environment-responsive (pH-responsive, redox-responsive and light-responsive, etc) groups into the co-delivery system. The antitumor activity was further improved. In the present paper, the environment- responsive delivery systems in the application of co-delivery gene and drug in recent years were reviewed, and their remarkable properties in the antitumor activity were analyzed and summarized.
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Co-delivery of paclitaxel and gene could achieve synergistic therapeutic effect, enhance therapeutic outcomes, reduce toxicity and reverse multiple drug resistance.Liposomes, nanoparticles and micells are usually used as the co-delivery systems of paclitaxel drugs and genes.We reviewed the progress in the co-delivery of paclitaxel and gene in the past few years by literature review, which would set a foundation for better clinical application of paclitaxel.
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Chemotherapy plays an important role in cancer treatment. However ,the low water-solubility and serious side effects are still the biggest obstacles in clinic. In addition,the wide use of chemotherapeutic drugs would result in the multidrug resis?tance(MDR)and the single chemotherapy could not meet the demand of clinic anymore. Combination therapy by two or more drugs used in the same time,has become the best choice for cancer patients. It not only enhances the cytotoxicity of the chemotherapeutic drugs due to the synergistic effect of the drugs,but also inhibits the MDR to improve uptake and cytotoxicity of the chemotherapeutic drugs when adding MDR inhibitors. The drug delivery system can improve the water-solubility due to the good biocompatibility of bio?degradable material which is the most property for drug delivery carriers. In addition,the targeting ability of the system and the con?trolled release of chemotherapeutic drugs can also reduce the side effects of drugs such as the cardiotoxicity of doxorubicin. The co-deliv?ery system loading two or more chemotherapeutic drugs in the same carrier can get better cytotoxicity than the combination therapy using free drugs due to the efficient delivery of chemotherapeutic drugs to cancer cells ,and are even better than the combination of single drug-loaded drug delivery systems because the chemotherapeutic drugs can get into the cancers cells in the same time. In addi?tion,with the rapid development of gene therapy,the co-delivery of drugs and genes has also been a hot topic these days. In this paper, we focus on the preparation,characteristics and application of drug+drug and drug+gene co-delivery system,which can produce the synergistic effects or inhibit the MDR of cancer cells.
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Chemotherapy plays an important role in cancer treatment. However, the low water-solubility and serious side effects are still the biggest obstacles in clinic. In addition, the wide use of chemotherapeutic drugs would result in the multidrug resistance (MDR)and the single chemotherapy could not meet the demand of clinic anymore. Combination therapy by two or more drugs used in the same time, has become the best choice for cancer patients. It not only enhances the cytotoxicity of the chemotherapeutic drugs due to the synergistic effect of the drugs, but also inhibits the MDR to improve uptake and cytotoxicity of the chemotherapeutic drugs when adding MDR inhibitors. The drug delivery system can improve the water-solubility due to the good biocompatibility of biodegradable material which is the most property for drug delivery carriers. In addition, the targeting ability of the system and the controlled release of chemotherapeutic drugs can also reduce the side effects of drugs such as the cardiotoxicity of doxorubicin. The co-delivery system loading two or more chemotherapeutic drugs in the same carrier can get better cytotoxicity than the combination therapy using free drugs due to the efficient delivery of chemotherapeutic drugs to cancer cells, and are even better than the combination of single drug-loaded drug delivery systems because the chemotherapeutic drugs can get into the cancers cells in the same time. In addition, with the rapid development of gene therapy, the co-delivery of drugs and genes has also been a hot topic these days. In this paper, we focus on the preparation, characteristics and application of drug+drug and drug+gene co-delivery system, which can produce the synergistic effects or inhibit the MDR of cancer cells.
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The efficacy of chemotherapeutic drug in cancer treatment is often hampered by drug resistance of tumor cells, which is usually caused by abnormal gene expression. RNA interference mediated by siRNA and miRNA can selectively knock down the carcinogenic genes by targeting specific mRNAs. Therefore, combining chemotherapeutic drugs with gene agents could be a promising strategy for cancer therapy. Due to poor stability and solubility associated with gene agents and drugs, suitable protective carriers are needed and have been widely researched for the co-delivery. In this review, we summarize the most commonly used nanocarriers for co-delivery of chemotherapeutic drugs and gene agents, as well as the advances in co-delivery systems.
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OBJECTIVE: To develop a polyethylene glycol (PEG) modified cationic liposomes for the co-delivery of siRNA and honokiol to improve tumor therapy. METHODS: The PEG-modified cationic liposomes were prepared by thin film hydration method. Honokiol was loaded in the liposomes with hydrophobic interaction and siRNA was loaded with electrostatic interaction. The optimal formulation was screened according to size, Zeta potential, entrapment efficiency and serum stability. The liposomes were characterized with cellular uptake and intracellular localization of siRNA. The pharmacodynamic effect of honokiol-loaded liposomes (LH) and hono-kiol-siRNA-loaded liposomes (LH-siRNA) were verified by inhibition of cancer cell growth. RESULTS: All the honokiol-loaded liposomes had an average particel size of about 100 nm with high drug entrapment efficiency. The optimal liposome formulation (N/P ratio of 5) exhibited the best cellular uptake. The results of pH-dependent hemolysis and intracellular localization suggested that the LH-siRNA had good ability of endosomal escape. In vitro cell growth experiments showed that both LH and LH-siRNA had good inhibition action on tumor cell growth based on the effects of honokiol and siRNA. CONCLUSION: The PEG-modified cationic liposomes can be a potential carrier for co-delivery of siRNA and honokiol to tumors.