Current drug delivery最新文献

Background: Gestational diabetes mellitus (GDM) poses significant risks during pregnancy for both mother and fetus. Adherence to oral antidiabetic medications, like glibenclamide (GB), can be challenging, necessitating novel drug delivery methods. Nanostructured lipid carriers (NLC) offer a promising approach by efficiently permeating the skin due to their small size and lipid-based composition.

Objective: This study aimed to develop and evaluate transdermal patches loaded with glibenclamide NLCs to treat GDM.

Methods: Glibenclamide NLCs were prepared using hot homogenization with ultrasonication and melt dispersion method. A central composite design was utilized to optimize the formulations. Transdermal patches containing optimized NLCs were developed using HPMC K 100 and Eudragit L polymers. The patches were evaluated for various parameters, and their pharmacokinetic and pharmacodynamic studies were carried out to assess their safety and efficacy.

Results: Optimized NLCs efficiently permeated rat skin. Cell viability studies indicated the nontoxicity of the formulations. NLC-loaded transdermal patches (F2 and F7) showed drug release of 1098 μg/cm² and 1001.83 μg/cm² in 24 h, with a 2.5-fold higher flux and permeation coefficient than the GB patch. Pharmacokinetic analysis revealed Tmax of 8 and 10 h and C_max of 7127 ng/ml and 7960 ng/ml for F2 and F7, respectively, ensuring sustained drug action. AUC0-α was 625681 ng/ml·h and 363625 ng/ml·h for F2 and F7, respectively, indicating improved bioavailability.

Conclusion: Transdermal patches incorporating NLCs hold promise for enhancing glibenclamide's therapeutic efficacy in GDM treatment. Improved skin permeation, sustained drug release, and enhanced bioavailability make NLC-based transdermal patches a potential alternative with better patient compliance.

Purpose: The aim of the study is to prepare entecavir (ETV)-loaded orodispersible films (ODFs) using polyvinyl alcohol (PVA)/polyethylene glycol (PEG) graft copolymer (Kollicoat® IR) as a film-forming agent, and further to evaluate the dissolution rate, mechanical and physicochemical properties of films.

Methods: ETV-ODFs were prepared by a solvent casting method. The amount of film-forming agent, plasticizer, and disintegrating agent was optimized in terms of the appearance, thickness, disintegration time and mechanical properties of ODFs. The compatibility between the drug and each excipient was conducted under high temperature (60 °C), high humidity (RH 92.5%), and strong light (4500 Lx) for 10 days. The dissolution study of optimal ODFs compared with the original commercial tablet (Baraclude®) was performed using a paddle method in pH 1.0, pH 4.5, pH 6.8, and pH 7.4 media at 37 °C. The morphology of ODFs was observed via scanning electron microscopy (SEM). The mechanical properties such as tensile strength (TS), elastic modulus (EM), and percentage elongation (E%) of ODFs were evaluated using the universal testing machine. The physicochemical properties of ODFs were investigated using X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FT-IR).

Results: The related substances were less than 0.5% under high temperature, high humidity, and strong light for 10 days when ETV was mixed with excipients. The optimal formulation of ODFs was set as the quality ratio of Kollicoat® IR, glycerol, sodium alginate (ALG-Na): TiO2: MCC+CMC-Na: ETV was 60:9:12:1:1:1. The drug-loaded ODFs were white and translucent with excellent stripping property. The thickness, disintegration time, EM, TS, and E% were 103.33±7.02 μm, 25.31±1.95 s, 25.34±8.69 Mpa, 2.14±0.26 Mpa, and 65.45±19.41 %, respectively. The cumulative drug release from ODFs was more than 90% in four different media at 10 min. The SEM showed that the drug was highly dispersible in ODFs, and the XRD, DSC, and FT-IR results showed that there occurred some interactions between the drug and excipients.

Conclusion: In conclusion, the developed ETV-loaded ODFs showed relatively short disintegration time, rapid drug dissolution, and excellent mechanical properties. This might be an alternative to conventional ETV Tablets for the treatment of chronic hepatitis B.

Background: Linagliptin (LNG) exhibits poor bioavailability and numerous side effects, significantly limiting its use. Transdermal drug delivery systems (TDDS) offer a potential solution to overcome the first-pass effect and gastrointestinal reactions associated with oral formulations.

Objective: The aim of this study was to develop LNG microparticle gels to enhance drug bioavailability and mitigate side effects.

Methods: Linagliptin hyaluronic acid (LNG-HA) microparticles were prepared by spray drying method and their formulation was optimized via a one-factor method. The solubility and release were investigated using the slurry method. LNG-HA microparticle gels were prepared and optimised using in vitro transdermal permeation assay. The hypoglycaemic effect of the LNG-HA microparticle gel was examined on diabetic mice.

Results: The results indicated that the LNG-HA microparticle encapsulation rate was 84.46%. Carbomer was selected as the gel matrix for the microparticle gels. Compared to the oral API, the microparticle gel formulation demonstrated a distinct biphasic release pattern. In the first 30 minutes, only 43.56% of the drug was released, followed by a gradual release. This indicates that the formulation achieved a slow-release effect from a dual reservoir system. Furthermore, pharmacodynamic studies revealed a sustained hypoglycemic effect lasting for 48 hours with the LNG microparticle gel formulation.

Conclusion: These findings signify that the LNG microparticle gel holds significant clinical value for providing sustained release and justifies its practical application.

Introduction/objective: To prolong the ocular residence time of gatifloxacin and enhance its efficacy against bacterial keratitis, this study developed a velocity-controlled polyethylene glycol-dithiothreitol-boric acid (PDB) hydrogel loaded with gatifloxacin.

Methods: First, the basic properties of the synthesized PDB hydrogel and the gatifloxacin-loaded PDB hydrogel were assessed. Secondly, the in vitro degradation rate of the drug-loaded PDB was measured in a simulated body fluid environment with pH 7.4/5.5. The release behavior of the drug-loaded PDB was studied using a dialysis method with PBS solution of pH 7.4/5.5 as the release medium. Finally, a mouse model of bacterial keratitis was established, and tissue morphology was observed using hematoxylin-eosin staining. Additionally, mouse tear fluid was extracted to observe the antibacterial effect of the gatifloxacin-loaded PDB hydrogel.

Results: The results showed that the PDB hydrogel had a particle size of 124.9 nm and a zeta potential of -23.3 mV, with good porosity, thermosensitivity, viscosity distribution, rheological properties, and high cell compatibility. The encapsulation of gatifloxacin did not alter the physical properties of the PDB hydrogel and maintained appropriate swelling and stability, with a high drug release rate in acidic conditions. Furthermore, animal experiments demonstrated that the gatifloxacin- loaded PDB hydrogel exhibited superior therapeutic effects compared to gatifloxacin eye drops and displayed strong antibacterial capabilities against bacterial keratitis.

Conclusion: This study successfully synthesized PDB hydrogel and developed a gatifloxacin drug release system. The hydrogel exhibited good thermosensitivity, pH responsiveness, stability, and excellent biocompatibility, which can enhance drug retention, utilization, and therapeutic effects on the ocular surface.

Niosomes are newly developed, self-assembling sac-like transporters that deliver medication at a specific site in a focused manner, increasing availability in the body and prolonging healing effects. Niosome discovery has increased drugs' therapeutic effectiveness while also reducing adverse effects. This article aims to concentrate on the increase in the worldwide utilization of niosomal formulation. This overview presents a thorough perspective of niosomal investigation up until now, encompassing categories and production techniques, their significance in pharmaceutical transportation, and cosmetic use. The thorough literature review revealed that extensive attention has been given to developing nanocarriers for drug delivery as they hold immense endeavor to attain targeted delivery to the affected area simultaneously shielding the adjacent healthy tissue. Many reviews and research papers have been published that demonstrate the interest of scientists in niosomes. Phytoconstituents, which possess antioxidant, antibiotic, anti-inflammatory, wound healing, anti-acne, and skin whitening properties, are also encapsulated into niosome. Their flexibility allows for the incorporation of various therapeutic agents, including small molecules, proteins, and peptides making them adaptable for different types of drugs. Niosomes can be modified with ligands, enhancing their targeting capabilities. A flexible drug delivery mechanism provided by non-ionic vesicles, which are self-assembling vesicular nano-carriers created from hydrating non-ionic surfactant, cholesterol, or amphiphilic compounds along comprehensive applications such as transdermal and brain-targeted delivery.

Immunomodulatory mechanisms are indispensable and key factors in maintaining the balance of the environment in humans. When the immune function of the immune system is impaired, autoimmune diseases occur. Excessive body fatigue, natural aging of the human body, malnutrition, genetic factors and other reasons cause low immune function, due to which the body is prone to being infected by bacteria or cancer. Clinically, the existing therapeutic drugs still have problems such as high toxicity, long treatment cycle, drug resistance and high price, so we still need to explore and develop a high efficiency and low toxicity drug. Poly(lactic-co-glycolic acid) (PLGA) refers to a nontoxic polymer compound that exhibits excellent biocompatibility. Traditional Chinese medicine (TCM) monomers come from natural plants, and have the characteristics of high efficiency and low toxicity. Applying PLGA to TCM monomers can make up for the defects of traditional dosage forms, improve bioavailability, reduce the frequency and dosage of drug use, and reduce toxicity and side effects, thus having the characteristics of sustained release and targeting. Accordingly, PLGA nanoparticles loaded with TCM monomers have been the focus of development. The previous research on drug loading advantages, preparation methods, and immune regulation of TCM PLGA nanoparticles is summarized in the following sections.

Introduction: In the present study, neuroprotective effects of berberine (BBR) and berberine nanomicelle (BBR-NM) against lipopolysaccharides (LPS)-induced stress oxidative were investigated, and compared by evaluating their antioxidant and anti-inflammatory activities in PC12 cells, and rat brains. A fast, green, and simple synthesis method was used to prepare BBR-NMs.

Method: The prepared BBR-NMs were then characterized using dynamic light scattering (DLS), transmission electron microscopy (TEM), and scanning electron microscopy (SEM). In vitro experiments were carried out on the LPS-treated PC12 cell lines to investigate the anti-cytotoxic and antioxidant properties of BBR-NM and BBR. The results showed that BBR-NMs with a diameter of ~100 nm had higher protective effects against ROS production and cytotoxicity induced by LPS in PC12 cells in comparison with free BBR.

Results: Moreover, in vivo experiments indicated that the activity levels of antioxidant enzymes, such as superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx), increased in the brain of LPS-treated rats administrated with BBR-NM at the optimum dose of 100 mg.kg^-1. BBR-NM administration also resulted in decreased concentration of lipid peroxidation (MDA) and pro-inflammatory cytokines, such as Serum interleukin-1 beta (IL-1β) and tumor necrosis factor-alpha (TNF-α).

Conclusion: Overall, BBR-NM demonstrated higher neuroprotective effects than free BBR, making it a promising treatment for improving many diseases caused by oxidative stress and inflammation.

The majority of deadly cancers that afflict the female reproductive system occur in the ovary. Around 1,40,000 women worldwide die from ovarian cancer each year, making it the sixth most common cancer-associated deceases among females in the United States. Modern, cutting-edge treatments like chemotherapy and surgery frequently produce full remissions, but the recurrence rate is still very high. When this crippling condition is diagnosed, there are frequently few therapeutic choices available because of how quietly it manifests. Healthcare practitioners must have a fundamental grasp of the warning signs and symptoms of ovarian cancer, as well as the imaging techniques and treatment choices available, to give the patient the best care possible. The discipline of medical nanotechnology has gained a lot of momentum in recent years in resolving issues and enhancing the detection and treatment of different illnesses, including cancer. This article gives a brief summary of types, risk factors and approaches to ovarian cancer treatment. We subsequently discussed the pathophysiology of ovarian cancer with the risk factors. This review also emphasizes the various signalling pathways involved in ovarian cancer. Our comprehensive integration of recent findings in fundamental research in the nano arena reveals the strong interest in these nanomedicines in ovarian cancer treatment. However, these nanomedicines still require more research, as indicated by the comparatively small number of clinical trials ongoing. This article will provide a reference for ovarian cancer treatment.

Background: Prostate cancer continues to be a serious danger to men's health, despite advances in the field of cancer nanotechnology. Although different types of cancer have been studied using nanomaterials and theranostic systems derived from nanomaterials, they have not yet reached their full potential for prostate cancer due to issues with in vivo biologic compatibility, immune reaction responses, accurate targetability, as well as a therapeutic outcome related to the nano-structured mechanism.

Method: The ultimate motive of this article is to understand the theranostic nanotechnology-based scheme for treating prostate cancer. The categorization of diverse nanomaterials in accordance with biofunctionalization tactics and biomolecule sources has been emphasized in this review so that they might potentially be used in clinical contexts and future advances. These opportunities can enhance the direct visualization of prostate tumors, early identification of prostate cancer-associated biomarkers at extremely low detection limits, and finally, the therapy for prostate cancer.

Result: In December 2022, a thorough examination of the scientific literature was carried out utilizing the Web of Science, PubMed, and Medline databases. The goal was to analyze novel applications of nanotechnology in the treatment of prostate cancer, together with their structural layouts and functionalities.

Conclusion: The various treatments and the reported revolutionary nanotechnology-based systems appear to be precise, safe, and generally successful; as a result, this might open up a new avenue for the detection and eradication of prostate cancer.

Cold atmospheric plasma (CAP) is an ionized matter with potential applications in various medical fields, ranging from wound healing and disinfection to cancer treatment. CAP's clinical usefulness stems from its ability to act as an adjustable source of reactive oxygen and nitrogen species (RONS), which are known to function as pleiotropic signaling agents within cells. Plasma-activated species, such as RONS, have the potential to be consistently and precisely released by carriers, enabling their utilization in a wide array of biomedical applications. Furthermore, understanding the behavior of CAP in different environments, including water, salt solutions, culture medium, hydrogels, and nanoparticles, may lead to new opportunities for maximizing its therapeutic potential. This review article sought to provide a comprehensive and critical analysis of current biomaterial approaches for the targeted delivery of plasma-activated species in the hope to boost therapeutic response and clinical applicability.