1.Research progress on lipid nanoparticle messenger RNA delivery system.
Journal of Zhejiang University. Medical sciences 2025;54(4):446-454
Messenger RNA (mRNA) therapeutics involve delivering in vitro transcribed mRNA into specific cells to produce target proteins for the treatment or prevention of diseases. However, the development of mRNA therapeutics relies largely on mRNA delivery systems. Lipid nanoparticles (LNPs) represent the most widely used mRNA carriers in clinical applications. Composed of ionizable lipids, zwitterionic phospholipids, cholesterol, and polyethylene glycol-lipids, LNPs can address critical challenges in mRNA drug development, such as poor in vivo stability and the difficulty in crossing biological barriers. Ultimately, LNPs enable safe, efficient, and targeted mRNA delivery to the liver, lung, spleen, and other organs. This review outlines the roles of the four lipid components in LNPs for mRNA delivery. It then introduces targeted mRNA delivery to various organs/tissues such as the liver, lung, spleen, pancreas, bone marrow, and placenta, using strategies such as antibody modification, lipid structure alteration, and specialized administration routes. Additionally, this review discusses the applications and challenges of LNP-based mRNA therapeutics in disease treatment, aiming to provide insights for the clinical translation of mRNA therapies and for further innovations in LNP delivery systems.
Humans
;
RNA, Messenger/administration & dosage*
;
Nanoparticles/chemistry*
;
Lipids/chemistry*
;
Drug Delivery Systems
;
Animals
;
Liposomes
2.Research progress of liposome drug delivery system in the treatment of head and neck cancer.
Bo LIU ; Yaqin TU ; Nan WU ; Hongjun XIAO
Journal of Clinical Otorhinolaryngology Head and Neck Surgery 2025;39(1):91-96
Head and neck tumors are one of the major diseases that threaten human health. Targeted chemotherapy is an important treatment for head and neck tumors. However, many anti-cancer drugs are difficult to reach effective concentrations in tumors and can cause damage to normal tissues. Therefore, the efficient delivery of anti-tumor drugs, improvement of their therapeutic effects, and reduction of their adverse effects on the whole body and locally are urgent issues in targeted drug research. Liposomes have been widely studied due to their unique characteristics, including amphiphilicity, biocompatibility, biodegradability, and low toxicity. This article outlines the current applications and prospects of liposome drug delivery systems in different treatment modalities for head and neck tumors in recent years, aiming to provide more options for the treatment of head and neck tumors.
Humans
;
Liposomes
;
Head and Neck Neoplasms/drug therapy*
;
Drug Delivery Systems
;
Antineoplastic Agents/administration & dosage*
3.Harmonizing tradition and technology: Liposomal nanocarriers unlocking the power of natural herbs in Traditional Chinese Medicine.
Ibrahim SHAW ; Aaron Albert ARYEE ; Yimer Seid ALI ; George Frimpong BOAFO ; Jingjing TIAN ; Ronald MLAMBO ; Songwen TAN ; Chuanpin CHEN
Chinese Journal of Natural Medicines (English Ed.) 2025;23(6):700-713
Natural herbs demonstrate significant therapeutic potential in managing chronic and complex diseases; however, their clinical application faces limitations due to low bioavailability, instability, toxicity, and herb-drug interactions. Furthermore, insufficient standardized evidence and global acceptance impede their widespread adoption. Liposomes, nanocarriers consisting of a phospholipid bilayer enclosing an aqueous core, present a promising approach for enhancing the pharmacokinetics and therapeutic efficacy of herbal compounds. These adaptable systems can encapsulate both hydrophilic and hydrophobic agents, enabling targeted drug delivery and enhanced stability. Moreover, liposomes can be modified to carry diagnostic and imaging agents, enabling precise disease detection and monitoring. While liposomes offer potential as an innovative delivery technology for herbal remedies, their application in Traditional Chinese Medicine (TCM) remains relatively unexplored. TCM, with its holistic, energy-based approach to health and organ function, presents distinct challenges regarding formulation and delivery. This review examines the therapeutic potential of herbal medicines, emphasizing how liposomes address delivery challenges within the TCM framework. It also investigates the integration of TCM with Western medical practices, demonstrating how liposomal systems may bridge these approaches. The review analyzes key formulation techniques for TCM-loaded liposomes, particularly the microfluidic method, which demonstrates superior control over particle size and encapsulation efficiency compared to conventional methods. The analysis addresses barriers to integrating liposomal delivery systems with TCM, including physicochemical properties, scalability issues, and regulatory challenges. Finally, this review provides strategic recommendations for overcoming these obstacles and identifies future research directions to maximize the potential of liposomal technology in enhancing TCM therapies.
Liposomes/chemistry*
;
Drugs, Chinese Herbal/administration & dosage*
;
Humans
;
Medicine, Chinese Traditional/methods*
;
Drug Delivery Systems
;
Drug Carriers/chemistry*
;
Animals
;
Nanoparticles/chemistry*
4.Advances of virus-like particles as mRNA delivery vectors.
Xinyu LIN ; Shuling REN ; Tingdong LI ; Shengxiang GE
Chinese Journal of Biotechnology 2025;41(4):1268-1279
With the continuous development of messenger RNA (mRNA) technology, mRNA-based drugs have shown broad application prospects in recent years. Since mRNA is easy to be degraded and difficult to enter cells directly, the mRNA delivery vectors have always been one of the focuses in the development of mRNA-based drugs. Although lipid nanoparticles (LNPs) have been widely used for the delivery of mRNA, they tend to accumulate in the liver, and repeated administration can easily induce inflammatory response which leads to tissue damage. Compared with LNPs, virus-like particles (VLPs) have the advantages of high biocompatibility and safety, being expected to offer new solutions for mRNA delivery. Based on the practical application requirements, this review summarized the research progress in VLPs according to the mRNA delivery steps: particle assembly, delivery into cells, and intracellular release. We hope to provide a basis and design ideas for the development of new VLPs as delivery vectors, promote the application of VLPs in mRNA delivery, and provide new possibilities for the research and application of mRNA-based therapeutics.
RNA, Messenger/administration & dosage*
;
Humans
;
Nanoparticles/chemistry*
;
Genetic Vectors
;
Lipids/chemistry*
;
Drug Delivery Systems/methods*
;
Virion
;
Animals
;
Gene Transfer Techniques
;
Liposomes
5.Observation of analgesic efficacy of liposomal bupivacaine for local infiltration anesthesia in unicompartmental knee arthroplasty: a prospective randomized controlled study.
Shanbin ZHENG ; Hongyu HU ; Tianwei XIA ; Liansheng SHAO ; Jiaqing ZHU ; Jiahao SUN ; Bowen MA ; Chiyu ZHANG ; Libing HUANG ; Xun CAO ; Zhiyuan CHEN ; Chao ZHANG ; Jirong SHEN
Chinese Journal of Reparative and Reconstructive Surgery 2024;38(12):1458-1465
OBJECTIVE:
A prospective randomized controlled study was conducted to investigate the early postoperative analgesic effectiveness of using liposomal bupivacaine (LB) for local infiltration anesthesia (LIA) in unicompartmental knee arthroplasty (UKA).
METHODS:
Between January 2024 and July 2024, a total of 80 patients with knee osteoarthritis (KOA) who met the selection criteria were enrolled in the study. Patients were randomly assigned to either the LB group or the "cocktail" group in a 1∶1 ratio using a random number table, with 40 patients in each group. Baseline characteristics, including gender, age, body mass index, operated side, Kellgren-Lawrence grade, and preoperative American Society of Anesthesiologists (ASA) classification, Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) score, and knee joint range of motion, showed no significant difference between the two groups ( P>0.05). Both groups received LIA and comprehensive pain management. The surgical duration, incision length, pain-related indicators [resting and activity visual analogue scale (VAS) scores, total dosage of oral morphine, WOMAC scores], knee joint range of motion, first ambulation time after operation, length of hospital stay, and postoperative adverse events.
RESULTS:
There was no significant difference between the two groups in surgical duration, incision length, first ambulation time after operation, length of hospital stay, total dosage of oral morphine, and pre-discharge satisfaction with surgery and WOMAC scores ( P>0.05). At 4, 12, and 24 hours after operation, the resting and activity VAS scores in the "cocktail" group were lower than those in the LB group; at 60 and 72 hours postoperatively, the resting VAS scores in the LB group were lower than those in the "cocktail" group, with the activity VAS scores also being lower at 60 hours; all showing significant differences ( P<0.05). There was no significant difference in the above indicators between the two groups at other time points ( P>0.05). On the second postoperative day, the sleep scores of the LB group were significantly higher than those of the "cocktail" group ( P<0.05), while there was no significant difference in sleep scores on the day of surgery and the first postoperative day ( P>0.05). Additionally, the incidence of complications showed no significant difference between the two groups ( P>0.05).
CONCLUSION
The use of LB for LIA in UKA can provide prolonged postoperative pain relief; however, it does not demonstrate a significant advantage over the "cocktail" method in terms of short-term analgesic effects or reducing opioid consumption and early functional recovery after UKA. Nevertheless, LB may help reduce postoperative sleep disturbances, making it a recommended option for UKA patients with cardiovascular diseases and insomnia or other mental health issues.
Aged
;
Female
;
Humans
;
Male
;
Middle Aged
;
Anesthesia, Local/methods*
;
Anesthetics, Local/administration & dosage*
;
Arthroplasty, Replacement, Knee/methods*
;
Bupivacaine/administration & dosage*
;
Liposomes
;
Osteoarthritis, Knee/surgery*
;
Pain Measurement
;
Pain, Postoperative/prevention & control*
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Prospective Studies
;
Treatment Outcome
6.Effects of intranasal administration of tripterygium glycoside-bearing liposomes on behavioral cognitive impairment of mice induced by central nervous system inflammation.
Min YAN ; Lan ZHANG ; Lu-Lu ZHANG ; Zhen-Qiang ZHANG ; Hua-Hui ZENG ; Xiang-Xiang WU
China Journal of Chinese Materia Medica 2023;48(9):2426-2434
Tripterygium glycosides liposome(TPGL) were prepared by thin film-dispersion method, which were optimized accor-ding to their morphological structures, average particle size and encapsulation rate. The measured particle size was(137.39±2.28) nm, and the encapsulation rate was 88.33%±1.82%. The mouse model of central nervous system inflammation was established by stereotaxic injection of lipopolysaccharide(LPS). TPGL and tripterygium glycosides(TPG) were administered intranasally for 21 days. The effects of intranasal administration of TPG and TPGL on behavioral cognitive impairment of mice due to LPS-induced central ner-vous system inflammation were estimated by animal behavioral tests, hematoxylin-eosin(HE) staining of hippocampus, real-time quantitative polymerase chain reaction(RT-qPCR) and immunofluorescence. Compared with TPG, TPGL caused less damage to the nasal mucosa, olfactory bulb, liver and kidney of mice administered intranasally. The behavioral performance of treated mice was significantly improved in water maze, Y maze and nesting experiment. Neuronal cell damage was reduced, and the expression levels of inflammation and apoptosis related genes [tumor necrosis factor-α(TNF-α), interleukin-1β(IL-1β), BCL2-associated X(Bax), etc.] and glial activation markers [ionized calcium binding adaptor molecule 1(IBA1) and glial fibrillary acidic protein(GFAP)] were decreased. These results indicated that liposome technique combined with nasal delivery alleviated the toxic side effects of TPG, and also significantly ameliorated the cognitive impairment of mice induced by central nervous system inflammation.
Mice
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Animals
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Tripterygium
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Liposomes
;
Glycosides/therapeutic use*
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Administration, Intranasal
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Lipopolysaccharides
;
Central Nervous System
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Cognitive Dysfunction/drug therapy*
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Inflammation/metabolism*
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Tumor Necrosis Factor-alpha/metabolism*
;
Cardiac Glycosides
7.Preparation and evaluation of four kinds of mixed essential oil liposomes in Jieyu Anshen Formula.
Yong-Mei GUAN ; Jia LIU ; Jian-Lin ZHANG ; Li-Hua CHEN ; Wei-Feng ZHU ; Zhen-Zhong ZANG ; Chen JIN ; Lu WU
China Journal of Chinese Materia Medica 2019;44(7):1363-1370
In order to increase the stability and solubility of essential oil in Jieyu Anshen Formula, this study was to prepare the essential oil into liposomes. In this experiment, the method for the determination of encapsulation efficiency of liposomes was established by ultraviolet spectrophotometer and dextran gel column. The encapsulation efficiency and particle size of liposomes were used as evaluation indexes for single factor investigation and Box-Behnken design-response surface method was used to optimize the design. Then the optimal formulation of volatile oil liposome was characterized using methyleugenol, elemin, β-asarone and α-asarone as index components. Finally, the in vitro transdermal properties of liposomes were studied by modified Franz diffusion cell. The results showed that the concentration of lecithin, the mass ratio of lecithin to volatile oil, and the stirring speed were the three most significant factors affecting the liposome preparation. The optimum formulation of volatile oil liposome was as follows: the concentration of lecithin was 7 g·L~(-1); mass ratio of lecithin to volatile oil was 5∶1; and the stirring speed was 330 r·min~(-1). Under such conditions, the prepared liposomes had blue emulsion light, good fluidity, half translucent, with particle size of(102.6±0.35) nm, Zeta potential of(-17.8±0.306) mV, permeability of(1.67±1.01)%, and stable property if liposome was stored at 4 ℃. 24 h after percutaneous administration, the cumulative osmotic capacity per unit time was(30.485 2±1.238 9),(34.794 8±0.928 3),(26.677 1±1.171 7),(3.066 2±0.175 3) μg·cm~(-2)respectively for methyleugenol, elemin, β-asarone and α-asarone. In vitro transdermal behaviors of methyleugenol, elemin, β-asarone and α-asarone in liposomes were all consistent with Higuchi equation. The prepared volatile oil liposomes met the relevant quality requirements, providing a reference for further research on preparation of multi-component Chinese medicine essential oil liposomes.
Administration, Cutaneous
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Drugs, Chinese Herbal
;
analysis
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Liposomes
;
Oils, Volatile
;
analysis
;
Particle Size
;
Solubility
8.Acute and chronic toxicity of 0.5% podophyllotoxin-loaded nanostructured lipid carriers to vaginal mucosa in rabbits and rats.
Lishi LIU ; Kai HAN ; Qi WANG ; Yan GAO ; Jingying WANG ; Kang ZENG
Journal of Southern Medical University 2018;38(12):1527-1532
OBJECTIVE:
To test the acute and chronic toxicity of topical application of 0.5% podophyllotoxin-loaded nanostructured lipid carriers (POD-NLC) to the vaginal mucosa.
METHODS:
Twelve New Zealand rabbits were randomized into 3 groups and subjected to daily topical applications of normal saline (control group), 0.5% podophyllotoxin tincture (POD-T) or 0.5% POD-NLC on the vaginal mucosa for 10 consecutive days, and the pathological changes in the mucosa were graded using the Eckstein scoring system.The acute toxicity of POD-NLC was tested in 20 SD female rats, which received intravaginal administration of POD-NLC or vehicle for 3 times within 24 h; After 14 days of continuous observation, the rats were dissected for calculating the viscera coefficient.For testing the chronic toxicity of POD-NLC, 80 SD female rats were randomized into 4 groups and subjected to daily intravaginal administration of the vehicle or POD-NLC at low, moderate or high doses for 13 consecutive weeks.The rats were weighed once a week and at the end of the experiment, 2/3 of the rats from each group were sacrificed to collect blood samples, calculate the viscera coefficient, and examine the pathological changes in the liver.The remaining 1/3 rats were observed for another 2 weeks without further drug treatment and the same examinations were performed.
RESULTS:
In the rabbits, 0.5% POD-NLC elicited only mild irritation while POD-T caused moderate irritation of the vaginal mucosa.In the acute toxicity test, the organ coefficients were comparable between the rats treated with the vehicle and POD-NLC (>0.05).Long-term intravaginal administration of POD-NLC did not produce significant changes in the behavior, activity, body weight, blood biochemical profiles or organ coefficient as compared with the vehicle control group (>0.05).
CONCLUSIONS
Intravaginal administration of 0.5% POD-NLC causes very mild irritation without obvious acute or chronic toxicity to the vaginal mucosa in rabbits and rats.
Administration, Intravaginal
;
Animals
;
Female
;
Liposomes
;
Mucous Membrane
;
drug effects
;
Nanostructures
;
toxicity
;
Podophyllotoxin
;
administration & dosage
;
toxicity
;
Rabbits
;
Random Allocation
;
Rats
;
Vagina
;
drug effects
9.Formulation and Efficacy of Liposome-encapsulated Afatinib for Therapy of Non-small Cell Lung Cancer.
Xiaoyan LV ; Junjing YIN ; Xiucheng YANG ; Sha LIU ; Kaoxiang SUN
Chinese Journal of Lung Cancer 2018;21(9):663-669
BACKGROUND:
Afatinib, a second-generation irreversible epidermal growth factor inhibitor receptor for the development of non-small cell lung cancer and secondary drug resistance, has low bioavailability and adverse reactions due to current oral administration. The aim of this study was to prepare a novel drug delivery system, afatinib liposome, and to establish a method for the determination of encapsulation efficiency.
METHODS:
Four different preparation methods were used to prepare afatinib liposomes, and the optimal preparation process was determined by comparing the encapsulation efficiency and particle size.
RESULTS:
It has been verified that sephadex microcolumn centrifugation can be used to purify afatinib liposomes, and UV spectrophotometry can be employed to determine the entrapment efficiency of liposomes. Among different preparation methods, the encapsulation efficiency of afatinib liposomes prepared by ammonium sulfate gradient method was 90.73% and the average particle size was 108.6 nm.
CONCLUSIONS
Ammonium sulfate gradient method can be successfully applied to prepare afatinib liposomes that performed higher encapsulation efficiency and smaller particle size. The UV spectrophotometry employed to determine the liposome encapsulation efficiency was easy operation and with high accuracy.
Afatinib
;
Capsules
;
Carcinoma, Non-Small-Cell Lung
;
drug therapy
;
Drug Compounding
;
methods
;
Liposomes
;
Lung Neoplasms
;
drug therapy
;
Quinazolines
;
administration & dosage
;
chemistry
;
therapeutic use
10.The antibacterial effect of fatty acids on Helicobacter pylori infection.
The Korean Journal of Internal Medicine 2016;31(1):30-35
Eradication of Helicobacter pylori is recommended for the management of various gastric diseases, including peptic ulcers and mucosa-associated lymphoid tissue lymphoma. Because of the increasing prevalence of antibiotic resistance, the eradication rates of antibiotic-based therapies have decreased. Therefore, alternative treatments should be considered. The antibacterial properties of fatty acids (FAs) have been investigated in various organisms, including H. pylori. Some FAs, particularly polyunsaturated FAs, have been shown to have bactericidal activity against H. pylori in vitro; however, their antibacterial effects in vivo remain controversial. Poor solubility and delivery of FAs may be important reasons for this discrepancy. Recently, a series of studies demonstrated the antibacterial effects of a liposomal formulation of linolenic acid against H. pylori, both in vitro and in vivo. Further research is needed to improve the bioavailability of FAs and apply them in clinical use.
Animals
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Anti-Bacterial Agents/administration & dosage/*therapeutic use
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Drug Delivery Systems
;
Fatty Acids/administration & dosage/*therapeutic use
;
Helicobacter Infections/diagnosis/*drug therapy/microbiology
;
Helicobacter pylori/*drug effects/pathogenicity
;
Humans
;
Liposomes
;
Treatment Outcome

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