Current drug delivery最新文献

Background: The prevalence of Non-alcoholic Fatty Liver Disease (NAFLD) is closely related to the increase of the incidence rate of obesity.

Aims: To find out the targets of celastrol on NAFLD with the treatment of celastrol-loaded liposomes (Cel-Lips).

Methods: Gene Expression Omnibus (GEO) data were used to compare the expression of differential genes in NAFLD patients with normal individuals. Celastrol was loaded into liposomes to improve its solubility, as well as, achieving a passive targeting effect on the liver to improve the availability, which also could delay the release rate of celastrol to prolong the action time and thus reduce the frequency of administration. Due to rarely reported molecular mechanisms of celastrol, with the help of network pharmacological analysis, the targets of celastrol acting on NAFLD were predictively analyzed.

Results: An association between NAFLD and lipid metabolism was detected in GEO data. Cel-Lips significantly alleviated NAFLD in vivo. Through network pharmacology, it was found that most of the action pathways of celastrol were related to lipid metabolism.

Conclusion: Celastrol has the potential to treat NAFLD, and its possible targets have been identified through network pharmacological screening, which provides a certain basis for the follow-up researches.

Purpose: This study aimed to develop and evaluate triptolide nanoemulsion gels (TP-NE gels) as a transdermal drug delivery system.

Methods: TP-NE was prepared and optimized via emulsification and the central composite design response surface method. The optimized TP-NE gel was evaluated in vitro and in vivo. TP-NE gel microstructure, in vitro and in vivo pharmacokinetics, and anti-rheumatoid arthritis effects were studied to evaluate the feasibility of its percutaneous administration.

Results: The Optimized TP-NE was observed using a Malvern Autosizer Nano ZS 90 inspection system and a transmission electron microscope (TEM). The nanoemulsion had an average size of 162.9 ± 0.281 nm, a polydispersity index of 0.272 ± 0.024, a zeta potential of -30.03 ± 2.01 mV, and mostly spherical and uniform morphology. In addition, the TP-NE gel pharmacokinetics, assessed via a skin-blood two-site synchronous microdialysis, revealed that TP was higher in the skin than in the blood. TP-NE gel is crucial in reducing knee edema, inhibiting inflammation, and treating rheumatoid arthritis by regulating tumor necrosis factor-alpha, interleukin-1β, and -6 levels.

Conclusion: The TP-NE gel is a promising local delivery method for rheumatoid arthritis (RA)-associated edema and inflammation and can serve as a prospective platform for percutaneous TP administration.

The blood-prostate barrier (BPB), a non-static physical barrier, stands as an obstacle between the prostate stroma and the lumen of the prostate gland tube. The barrier has the ability to dynamically regulate and strictly control the mass exchange between the blood and the prostate, thereby limiting drug penetration into the prostate. The basement membrane, fibrous stromal layer, capillary endothelial cell, prostatic ductal epithelial cell, lipid layer, etc., have been confirmed to be involved in the composition of the barrier structure and altered membrane permeability mainly by regulating the size of paracellular ion pores. Various studies have been conducted to improve the efficiency of drug therapy for prostate diseases by changing the administration approaches, improving barrier permeability and increasing drug penetration. To gain a full understanding of BPB, the composition of BPB, the methodology for evaluating the permeability of BPB and alterations in barrier function under pathological conditions are summarized in this review. To find a shortcut for drug delivery across BPB, the biodistribution of drugs in the prostate and different methods of improving drug penetration across BPB are outlined. This review offers an applied perspective on recent advances in drug delivery across BPB.

Because of low immunogenicity, ease of modification, and inherent biosafety, peptides have been well recognized as vehicles to deliver therapeutic agents to targeted regions with improved pharmacokinetic characteristics. Enzyme-responsive self-assembled peptides (ERSAPs) show superiority over their naive forms due to their enhanced targeting efficacy and long-retention property. In this review, we have summarized recent advances in the therapeutic application of ERSAPs, mainly focusing on their self-therapeutic properties and potential as vehicles to deliver different drugs.

Since the authors are not responding to the editor’s requests to fulfill the editorial requirement, therefore, the article has beenwithdrawn of the journal "Current Drug Delivery".

Bentham Science apologizes to the readers of the journal for any inconvenience this may have caused.

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Background: Melanoma is a malignant skin cancer type with a high lethality rate due to active metastasis. Among the risk factors for its development is exposure to ultraviolet radiation (UV) and phenotypical characteristics such as clear skin and eyes. Given the difficulties of the conventional therapy, the high cost of the treatment and the low bioavailability of drugs, it is important to develop new therapeutic methods to circumvent this situation. Nanosystems such as micelles, liposomes and nanoparticles present advantages when compared to conventional treatments.

Objective: The objective of this paper is to carry out a literature review based on articles that dealt with the use of siRNA-loaded nanosystems for the treatment of melanoma, with trials carried out in vivo to assess tumor size.

Methods: The search was conducted in the Web of Science and PubMed databases considering the last 5 years, that is, the period between January 2017 to December 2021. The "SiRNA and Drug Delivery Systems and Melanoma" keywords were used in both databases, and the articles were analyzed using the inclusion and exclusion criteria established for this paper.

Results: The results obtained indicated that using siRNA transported via nanosystems was capable of silencing the BRAF tumor genes and of reducing tumor size and weight, not presenting in vitro and/or in vivo toxicity.

Conclusion: Such being the case, the development of these systems becomes a non-invasive and promising option for the treatment of melanoma.

Since the authors are not responding to the editor’s requests to fulfill the editorial requirement, therefore, the article has beenwithdrawn.

Bentham Science apologizes to the readers of the journal for any inconvenience this may have caused.

The Bentham Editorial Policy on Article Withdrawal can be found at https://benthamscience.com/editorial-policies-main.php.

Bentham science disclaimer: It is a condition of publication that manuscripts submitted to this journal have not been published and will not be simultaneouslysubmitted or published elsewhere. Furthermore, any data, illustration, structure or table that has been published elsewheremust be reported, and copyright permission for reproduction must be obtained. Plagiarism is strictly forbidden, and by submittingthe article for publication the authors agree that the publishers have the legal right to take appropriate action against theauthors, if plagiarism or fabricated information is discovered. By submitting a manuscript the authors agree that the copyrightof their article is transferred to the publishers if and when the article is accepted for publication.

Background This study aimed to improve the sustained and controlled release of glycyrrhizic acid to the infected site of Staphylococcus aureus small colony variants (SCVs). Methods The glycyrrhizic acid-loaded chitosan composite nanogel was prepared by inclusion action, Schiff's base formation, and electrostatic action. Furthermore, the formulation screening, characteristics, in vitro release, and antibacterial activity of the glycyrrhizic acid composite nanogel were explored. Results The final optimal formula comprised 10 mg/mL (chitosan) and 50 μL (glutaraldehyde). The loading capacity, encapsulation efficiency, mean size, polydispersity index, and zeta potential were 8.8%±1.6%, 92.1%±2.8%, 478.3±2.8 nm, 0.37±0.10, and 25.3±3.6 mv, respectively. Scanning electron microscope images showed a spherical shape with a relatively uniform distribution. The in vitro release study showed that glycyrrhizic acid composite nanogel exhibited a biphasic pattern with a sustained release of 52.1%±2.0% at 48 h in the pH 5.5 PBS. The minimum inhibitory and minimum biofilm inhibitory concentrations of glycyrrhizic acid composite nanogel against SCVs were 0.625 μg/mL. The time-killing curves and live/dead bacterial staining showed that glycyrrhizic acid composite nanogel had a stronger curative effect against SCVs strain with concentration-dependent. Conclusion This study provides promising glycyrrhizic acid composite nanogel to improve the treatment of SCV infection.

Background: 5-azacitidine is a very potent chemotherapeutic agent that suffers from certain disadvantages.

Objective: This study aims to prepare gold nanoparticles as a new nano-formula of 5-azacitidine that can improve its bioavailability and decrease its side effects.

Methods: 5-azacytidine-loaded GA-AuNPs were prepared and characterized by UV-Vis spectroscopy, infrared (IR), and electronic transmission microscope (TEM). This new platform was characterized in vitro by measuring its zeta potential, particle size, and drug loading efficacy, and the anti-proliferative effect on the MCF-7 cell line was evaluated. In vivo biodistribution studies of ^99mTc-5-aza solution and ^99mTc-5-aza-gold nano formula were conducted in tumor-bearing mice by different routes of administration (intravenous and intra-tumor).

Results: 5-Aza-GA-AuNPs formula was successfully prepared with an optimum particle size of ≈34.66 nm, the zeta potential of -14.4 mV, and high entrapment efficiency. ^99mTc-5-Aza-GA-AuNPs were successfully radiosynthesized with a labeling yield of 95.4%. Biodistribution studies showed high selective accumulation in tumor and low uptake in non-target organs in the case of the 5-Aza-GA-AuNPs formula than the ^99mTc-5-azacitidine solution.

Conclusion: ^99mTc-5-Aza-GA-AuNPs improved the selectivity and uptake of 5-azacitidine in cancer. Moreover, ^99mTc-5-Aza-GA-AuNPs could be used as hopeful theranostic radiopharmaceutical preparation for cancer.