Current drug delivery最新文献

Objective: DSPE-mPEG2000 is a phospholipid and polyethylene glycol conjugate used in various biomedical applications, including drug delivery, gene transfection, and vaccine delivery. Due to the hydrophilic and hydrophobic properties of DSPE-mPEG2000, it can serve as a drug carrier, encapsulating drugs in liposomes to enhance stability and efficacy.

Method: In this study, long-circulating podophyllotoxin liposomes (Lc-PTOX-Lps) were prepared using DSPE-mPEG2000 as a modifying material and evaluated for their pharmacokinetics and anticancer activity.

Result: Lc-PTOX-Lps had an encapsulation rate of 87.11±1.77%, an average particle size of 168.91±7.07 nm, a polydispersity index (PDI) of 0.19±0.04, and a zeta potential of -24.37±0.36 mV. In vitro release studies showed that Lc-PTOX-Lps exhibited a significant slow-release effect. The long-circulating liposomes demonstrated better stability compared to normal liposomes and exhibited a significant slow-release profile. Pharmacokinetic studies indicated that Lc-PTOX-Lps had a prolonged half-life, reduced in vivo clearance, and improved bioavailability. Additionally, Lc-PTOX-Lps exhibited better anticancer effects on MCF-7 cells and lower toxicity to normal cells compared to PTOX.

Conclusion: Lc-PTOX-Lps were synthesized using a simple and effective method, and Lc-PTOXLps are promising anticancer agents.

Background: Eczema, an inflammatory skin disease causing intense itching, is a function of a range of internal and external factors, impacting individuals of all ages and leading to economic loss. Inflammation is the most important manifestation of eczema, and Matricaria recutita essential oil (MREO) extracted from Matricaria recutita possesses excellent antibacterial and anti-inflammatory properties.

Methods: In this study, Matricaria recutita microemulsions were prepared by the trans-phase emulsification method and their stability was determined by evaluating the relevant indexes. Establishment of 2,4-dinitro-chlorobenzene-induced AD model in mice. Detection of serum indexes of IL-6, IL-17, and TNF-α, and on pathological tissue sections, the HE staining, toluidine blue staining, immunohistochemistry, and observation were performed.

Results: The study obtained optimal conditions for the preparation of microemulsion formulations of Matricaria recutita. Through quality evaluation, it was found that the microemulsion increased stability, reduced irritation, and retained anti-inflammatory activity and therapeutic effects on eczema compared to Matricaria recutita essential oil (MREO). Studies have demonstrated that microemulsion formulations of Matricaria recutita and Matricaria recutita significantly down regulate the proinflammatory factors TNF-α, IL-17, and IL-6. It was shown by hematoxylin-eosin (HE) staining that both Matricaria recutita essential oil (MREO) and Matricaria recutita microemulsion (MRME) improved the inflammatory status of eczematous skin tissues in mice. The number of mast cells expressed in the tissues was decreased in the surface-treated group, as shown by toluidine blue staining. Additionally, the number of mast cells expressed in the tissues in the surface-treated group was reduced, as demonstrated by immunohistochemistry. Furthermore, immunohistochemistry revealed that MREO and MRME have immunomodulatory effects on the tissues.

Conclusion: The study showed that microemulsion formulations of Matricaria recutita may serve as a novel remedy for eczema.

Introduction: The last strategy in targeted drug delivery systems is to deliver the anticancer drug to the tumor tissue to increase its therapeutic effect and minimize its undesirable side effects. In line with this goal in this research, the redox/pH-responsive disulfide magnetic nanocarriers based on PF127-NH₂/L-cysteine-CM-β-CD-FA were synthesized and evaluated in a doxorubicin delivery system.

Methods: We effectively surrounded Fe₃O₄ nanoparticles with SiO₂ using the sol-gel method, and then confidently coated them with oleic acid on Fe₃O₄@SiO₂ nanoparticles.. In another reaction, a PF127-NH₂/L-cysteine-CM-β-CD-FA was synthesized. The process involved modifying pluronic F127 (PF 127) with maleic anhydride and aminating it to form PF127-NH₂. The obtained PF127-NH₂ was attached to L-cysteine, followed by condensing with carboxymethyl-β-cyclodextrin and then functionalized by folic acid. Finally, PF127-NH₂/L-cysteine-CM-β-CD-FA was coated on the surface of magnetic nanoparticles, and the resulting PF127-NH₂/L-cysteine-CM-β-CD-FA was disulfidated to form the final nanocarrier network, which was abbreviated as LCMNPs-SS. The doxorubicin was used as a model drug and loaded into the LCMNPs-SS nanocarrier.

Results: The LCMNPs-SS nanocarrier exhibited excellent properties for controlled release, with a well-defined release rate, a controllable level by an external magnet, and adjusting by DLdithiothreitol concentration. The LCMNPs-SS nanocarrier could also break apart when exposed to an oxidant or a change in pH. This meant that the drug release could be fine-tuned in response to temperature, pH, or more than one stimulus.

Conclusion: These drug-carrying systems are valuable in reducing the dose of doxorubicin. High internalization of the synthesized LCMNPs-SS caused sped cellular uptake.

Conjugated Linoleic Acid (CLA) is a polyunsaturated dietary fatty acid. Probiotics can biohydrogenate CLA with multiple health benefits, especially in cancer treatment. In vitro, in vivo, and clinical studies have confirmed CLA isomers to possess anti-cancer activity. CLA has demonstrated its potential as an alternative treatment for cancer and also used as an adjuvant to reduce the side effects of existing treatment methods. The mechanism of the anticancer activity of CLA is still not clear; however, it may involve intervention with the cell cycle and modulation of gene expression. A greater potential of CLA for cancer treatment has been supported by more and more clinical trials to evaluate its potential. Some advanced technologies are in progress to overcome the flaws of current methods and enhance the microbial production of CLA. In conclusion, nutritional enrichment as a functional food and direct consumption of CLA may contribute to cancer management.

Objective: Angiogenesis is the process of forming new blood vessels from pre-existing vessels and occurs during development, wound healing, and tumor growth. In this review, we aimed to present a comprehensive view of various factors contributing to angiogenesis during carcinogenesis. Anti-angiogenesis agents prevent or slow down cancer growth by interrupting the nutrients and blood supply to the tumor cells, and thus can prove beneficial for treatment.

Method: The discovery of several novel angiogenic inhibitors has helped to reduce both morbidity and mortality from several life-threatening diseases, such as carcinomas. There is an urgent need for a new comprehensive treatment strategy combining novel anti-angiogenic agents for the control of cancer. The article contains details of various angiogenic inhibitors that have been adopted by scientists to formulate and optimize such systems in order to make them suitable for cancer.

Results: The results of several researches have been summarized in the article and all of the data support the claim that anti-angiogenic agent is beneficial for cancer treatment.

Conclusion: This review focuses on novel antiangiogenic agents that play a crucial role in controlling carcinogenesis.

Background: Breast cancer remains a significant global health challenge, with thymoquinone showing promise as a therapeutic agent, but hindered by poor solubility.

Objective: This study aimed to enhance TQ delivery to MCF-7 breast cancer cells using mesitylene- mesoporous silica nanoparticles coated with liposomes, designed for controlled drug release.

Methods: Nanoparticles were synthesized using the sol-gel method and coated with phosphatidylserine- cholesterol liposomes. Different nanocharacterization techniques and in vitro assays were employed to assess the drug release kinetics, cellular uptake, cytotoxicity, and apoptosis.

Results: The nanoparticles exhibited favorable properties, including a large pore size of 3.6 nm, a surface area of 248.96 m2/g, and a hydrodynamic size of 171.571 ± 8.342 nm with a polydispersity index of 0.182 ± 0.017, indicating uniformity and stability. The successful lipid bilayer coating was confirmed by a zeta potential shift from +6.25 mV to -5.65 mV. The coated nanoparticles demonstrated a slow and sustained drug release profile, with cellular uptake of FITC-formulated nanoparticles being approximately 5-fold higher than free FITC (P < 0.0001). Cytotoxicity assays revealed a significant reduction in cell viability (P < 0.0001), reaching an IC50 value of 25 μM at 48 hours. Apoptosis rates were significantly higher in cells treated with the formulated TQ compared to the free drug and control at both 24 and 48 hours (P < 0.0001).

Conclusion: This nanoformulation significantly enhanced TQ delivery, offering a promising strategy for targeted breast cancer therapy. Further preclinical studies are recommended to advance this approach in cancer treatment.

Background: Cancer treatment often involves the use of potent antineoplastic drugs like Capecitabine (CAP), which can lead to serious toxicities. There is a need for dosage forms to manage these toxicities that can deliver the medication effectively to the target site while maintaining therapeutic efficacy at lower doses. To achieve the aforesaid objective, NLC containing capecitabine (NANOBIN) was prepared and evaluated. Different formulations of NANOBIN, denoted as CaTS, CaT1S, CaT2S, CaTS1, and CaTS2, were designed and evaluated to improve drug delivery and therapeutic outcomes.

Methods: The NANOBIN formulations were prepared using the hot homogenization method. The characterization of these formulations was conducted based on various parameters such as particle size, Polydispersity Index (PDI), Zeta Potential (ZP), Transmission Electron Microscopy (TEM) imaging, and Encapsulation Efficiency (EE). In vitro evaluations included stability testing, release studies to assess drug release kinetics, and a cytotoxicity assay (MTT assay) to evaluate the efficacy of these formulations against human breast cancer cells (MCF-7).

Results: The characterization results revealed that all NANOBIN formulations exhibited particle sizes ranging from 65 to 193 nm, PDI values within the range of 0.26-0.37, ZP values between 46.47 to 61.87 mV (-ve), and high EE percentages ranging from 94.121% to 96.64%. Furthermore, all NANOBIN formulations demonstrated sustained and slow-release profiles of CAP. The MTT assay showed that the NANOBINs exhibited significantly enhanced cytotoxic efficacy, approximately 10 times greater than free CAP when tested on MCF-7 cells. These findings indicate the potential of NANOBINs to deliver CAP effectively to the target site, enabling prolonged drug availability and enhanced therapeutic effects at lower doses.

Conclusion: The study demonstrates that NANOBINs can effectively deliver CAP to target sites, prolonging drug exposure and enhancing therapeutic efficacy while reducing the required dose. Further studies are necessary to validate these findings and establish NANOBINs as a preferred treatment option for cancer therapy.

Objective: This study aimed to develop an emulgel containing minoxidil as a drug for hair growth promotion in diseases, such as androgenetic alopecia, using gelling agents, such as chitosan and fucoidan.

Methods: In this study, gelling agents were selected for the emulgel formulation. By various evaluation tests and through optimization, the chitosan-fucoidan combination was selected as the gelling agent for the preparation of emulgel using various evaluation parameters.

Results: X2, the best emulgel formulation, contained 2.54 % chitosan and 0.896 % fucoidan. Chitosan prolonged the duration of drug release, and controlled release was obtained. Fucoidan increased the gelling activity, water absorption rate, and stability of the formulation. In this study, the X2 formulation showed the highest percentage of drug release at the 12th hour. It was found to be 99.7%, which followed the zero-order release model.

Conclusion: Owing to the wide range of biological activities of fucoidan, the loaded active substance can be protected, and at the same time, its potency can be improved, resulting in effective treatment. Because fucoidan has diverse properties and potential, it will be widely used in the biomedical and pharmaceutical industries in the future.

Introduction/background: Tetrandrine (TET) has multiple pharmacological activities, but its water solubility is poor, which is the main reason for its low bioavailability.

Objectives: The purpose of this study was to prepare TET nanocrystals (TET-NCs) using a grinding method to enhance the dissolution rate and ultimately improve the bioavailability of TET.

Methods: TET-NCs were synthesized via media milling, employing Poloxam 407 (P407) as surface stabilizer and mannitol as a cryoprotectant during freeze-drying. The crystal structure, particle diameter, and zeta potential were characterized using differential scanning calorimetry (DSC), Fouriertransform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), and X-ray diffraction (XRD). The in vitro release behavior and pharmacokinetics of TET-NCs were assessed. The cytotoxicity of TET and TET-NCS on RAW264.7 cells was determined by the CCK-8 method.

Results: The particle size of TET-NCs was 360.0±7.03 nm, PDI was 0.26±0.03, and zeta potential was 6.64±0.22 mV. The cumulative dissolution within 60 minutes was 96.40±2.31%. The pharmacokinetic study showed that AUC0-72 h and Cmax of TET-NCs were significantly enhanced by 3.07 and 2.57 times, respectively, compared with TET (p<0.01). TET-NCs significantly increased the cell inhibition on RAW264.7 cells compared to the TET (P<0.01).

Conclusion: The preparation of TET-NCs enhanced dissolution rate and bioavailability significantly, and it also improved the inhibition effect of RAW264.7 cells.

Background: Plant-derived extracellular vesicles (PDEVs) are vital for intercellular material exchange and information transfer. They significantly regulate cellular functions, tissue repair, and self-defense mechanisms.

Objective: This review summarizes the formation pathways, composition, and potential applications of PDEVs in anti-tumor research and drug delivery systems.

Methods: We conducted a literature search using keywords such as "plant-derived extracellular vesicles," "exosomes," "drug delivery," "isolation and purification," "stability," "anti-tumor," and "tumor therapy" in databases including PubMed, Web of Science, and Scopus. We examined studies on the formation pathways of PDEVs, including fusion of multivesicular bodies with the plasma membrane, exosome-positive organelles, and vacuole release. We also reviewed isolation and purification techniques critical for studying their biological functions. Furthermore, we analyzed research on the application of PDEVs in cancer therapy, focusing on their inhibitory effects in various cancer models and their role as carriers in drug delivery systems.

Results: PDEVs have demonstrated potential in anti-tumor research, particularly with vesicles from plants like tea, garlic, and Artemisia annua showing inhibitory effects in breast, lung, and gastric cancer models. Additionally, PDEVs serve as effective carriers in drug delivery systems, offering possibilities for developing ideal therapeutic solutions.

Conclusion: While PDEVs show promise in cancer treatment and drug delivery, challenges such as standardization, storage stability, and elucidation of action mechanisms remain. Further research is needed to overcome these challenges and advance the clinical translation of PDEVs.