Current drug delivery最新文献

Background: Rheumatoid arthritis is a chronic autoimmune disease, progressively distinctive via cartilage destruction, auto-antibody production, severe joint pain, and synovial inflammation. Nanotechnology represents one of the utmost promising scientific technologies of the 21st century. Nanocarriers could be the key to unlocking its potential by encapsulating Rutin in targeted drug delivery systems, potentially for targeted Rheumatoid arthritis therapy.

Objective: The rationale of current research is to prepare liposomes loaded with a bioflavonoid drug rutin for effective management of rheumatoid arthritis.

Materials and methods: This study investigated the formulation of rutin liposomes using the thinfilm hydration technique, also known as the Bangham method. A Box-Behnken design was employed to optimize the formulation parameters. The LP2 batch was then characterized for its mean particle size, zeta potential, shape, diffraction pattern, and thermal properties. Finally, the in-vitro anti-oxidant and anti-inflammatory potential of the rutin liposomes were evaluated using appropriate assays.

Results: Out of thirteen batches, LP2 was found to be an optimized batch with a mean particle size of 167.1 nm, zeta potential -13.50 mV, and entrapment efficiency of 61.22%. The above results showed higher stability of rutin liposomes. Further characterization of LP2 for morphological assessment, XRD analysis, and DSC revealed its spherical shape less than 1 μm, polycrystalline nature, and thermographic peak at 139°C, respectively. Evaluation of the antioxidant properties and antiinflammatory potential of LP2 revealed its maximum therapeutic potential in the reduction of inflammation and protein denaturation when evaluated via in-vitro assays.

Conclusion: Rutin liposomal formulation has tremendous potential for the management of Rheumatoid arthritis due to its enhanced bioavailability, anti-oxidant, and anti-inflammatory properties when compared to free rutin.

Introduction: Assessing the cytotoxicity of gold nanoparticles (GNPs) has gained importance due to their development in the biomedical field.

Method: In this study, we systematically synthesized gold nanorods (GNRs), gold nanobipyramids (GNBPs), and gold nanocups (GNCs) using a seed-mediated method, with an average length of 32.53 ± 4.67 nm, 72.90 ± 7.54 nm and 118.01 ± 11.02 nm, respectively.

Results: Furthermore, using the cell counting kit-8 (CCK-8) assay, we assessed the cellular cytotoxicity of three different types of GNPs with various different surface coatings, such as organic cetyltrimethylammonium bromide (CTAB) and polyethylene glycol (PEG). The results showed that the cytotoxic behavior of GNPs was shape-dependent in the concentration range of 3.125 -100 μg/mL. The types of GNPs and their surface coating had a significant impact on how the GNPs behaved in cells. Compared to PEG-coated GNPs, which do not induce cell injury, CTAB-coated GNPs show more noticeable cytotoxicity.

Conclusion: Furthermore, compared to GNCs, the toxicity of GNRs and GNBPs against GES-1 cells, RAW 264.7 cells and LX-2 cells was greater. Our research provides an important new understanding of the effects of surface modification on the biocompatibility and the shape of GNPs in the biomedical field.

Pharmaceutical giants (e.g., Ashland, Bausch & Lomb, Johnson & Johnson, Medtronic, Neurelis, etc.) promote the growth of hydrogels globally. Hydrogel-based drug delivery system (DDS) market size accounted for USD 6415 million in 2021 and is estimated to reach USD 12,357 million by 2030, with a compound annual growth rate (CAGR) of 7.6% from 2022 to 2030. Hydrogels, characterized by their unique three-dimensional networks of hydrophilic polymers, have emerged as a keystone in the advancement of biomaterial science. Existing trends in the advancement of hydrogel drug delivery systems (DDS) involve the release of drugs in response to specific triggers such as pH, temperature, or enzymes for targeted drug delivery and to reduce the potential for systemic toxicity. They excel in their ability to achieve high drug loading capacities, their ease of manufacturing, and their inherent biocompatibility and biodegradability. These attributes not only promise crucial mechanistic features but also offer robust protection for labile drugs and enable the encapsulation of multiple therapeutic agents. Thus, hydrogels stand as promising candidates in various biomedical and pharmaceutical applications, ensuring controlled release and compatibility essential for therapeutic efficacy. Additionally, hydrogels have massive applications in tissue engineering, wound healing, cosmetics, and biomaterials (e.g., contact lenses and implantable devices). Furthermore, hydrogels possess the capability to release active drug(s) under sustained conditions as recommended. Their exceptional qualities position hydrogels as a preferred choice on a global scale. Moreover, they enhance bioavailability, optimize dosage regimens, promote patient compliance, and minimize adverse effects. Furthermore, hydrogels are recommended for use in clinical trials to enhance therapeutic drug delivery outcomes. Despite their remarkable properties, hydrogels do have certain disadvantages, including expensive manufacturing costs and incompatibility with certain drugs. The author has highlighted the fundamental ideas about hydrogels, their classification, global scenario, current developments in the field, and their potential applications. Overall, hydrogel application is progressing rapidly, toward more proficient and effective DDS in the future.

Background: Pancreatic cancer is a highly malignant tumor with a poor prognosis, and current treatment methods have limited effectiveness. Therefore, developing new and more effective therapeutic strategies is crucial. This study aims to establish pH-responsive silk fibroin (SF) nanoparticles encapsulating β-hydroxyisovalerylshikonin (SF@β-HIVS) to enhance the therapeutic effects against pancreatic cancer.

Methods: SF@β-HIVS nanoparticles were prepared using a self-assembly technique and characterized under different pH conditions using scanning electron microscopy (SEM) and dynamic light scattering (DLS). The effects of SF@β-HIVS on the viability, apoptosis, and migration of PANC-1 cells were assessed through in vitro experiments. Additionally, in vivo experiments using a PANC-1 xenograft mouse model evaluated the antitumor activity and biosafety of SF@β-HIVS.

Results: SF@β-HIVS nanoparticles exhibited a uniformly distributed spherical structure under pH 7.4 conditions and rapidly disintegrated in acidic environments, releasing the drug. In vitro experiments demonstrated that SF@β-HIVS significantly inhibited PANC-1 cell proliferation, induced apoptosis, and suppressed cell migration. In vivo, experiments confirmed the significant antitumor activity and good biosafety of SF@β-HIVS.

Conclusion: This study successfully developed pH-responsive SF@β-HIVS nanoparticles and validated their potential in treating pancreatic cancer. These findings provided a foundation for the clinical application of SF@β-HIVS in pancreatic cancer treatment.

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: 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.

Plant bioactive are being used since the early days of medicinal discovery for their various therapeutic activities and are safer compared to modern medicines. According to World Health Organization (WHO), approximately 180,000 deaths from burns occur every year with the majority in countries. Recent years have witnessed significant advancements in this domain, with numerous plant bioactive and their various nanoformulations demonstrating promising preclinical burn wound healing activity and identified plant-based nanotechnology of various materials through some variations of cellular mechanisms. A comprehensive search was conducted on scientific databases like PubMed, Web of Science, ScienceDirect and Google Scholar to retrieve relevant literature on burn wound, plants, nano formulations and in vivo studies from 1990 to 2024. From a total of approximately 180 studies, 40 studies were screened out following the inclusion and exclusion criteria, which reported 40 different plants and plant extracts with their various nano-formulations (NFs) that were used against burn wounds preclinically. This study provides the current scenario of naturally-derived targeted therapy, exploring the impact of natural products on various nanotechnology in burn wound healing on a preclinical model. This comprehensive review provides the application of herbal nanoformulations (HBNF) for the treatment of burn wounds. Natural products and their derivatives may include many unidentified bioactive chemicals or untested nano-formulations that might be useful in today's medical toolbox. Mostly, nano-delivery system modulates the bioactive compound's effectiveness on burn wounds and increases compatibility by suppressing inflammation. However, their exploration remains incomplete, necessitating possible pathways and mechanisms of action using clinical models.

Diabetic Foot Ulcer (DFU) is a chronic wound, and a person with diabetes has an increased lifetime risk of foot ulcers (19%-34%) and high morbidity (65% recurrence in 3-5 years, 20% lifetime amputation). Recent data have shown rising amputation rates, especially in the younger and minority populations. This abstract discusses innovative approaches for addressing this issue. This highlights the use of nanotechnology-based drug nanocomposite systems for natural wound healing therapies, with a focus on nanoparticles, nano-emulsions, and nanogels. This review also emphasizes the potential of hydrogels for drug delivery, highlighting their versatility in various medical applications. Furthermore, it delves into the use of silver nanoparticles (AgNP's) for treating diabetic wounds while acknowledging the need to address potential toxicity concerns. Finally, the abstract discusses the utilization of traditional herbal medicine and the integration of modern science to advance wound care, particularly focusing on wound microbiome, immune response, and controlled herbal medicine delivery. This study also highlights clinical trials conducted on DFU. Overall, these abstracts highlight the importance of exploring diverse and innovative solutions to chronic wound management.

Nanostructured lipid carriers (NLCs) are lipidic nanocarriers that recover the permanency and capacity of drug payloads. NLCs are well-known as second-generation lipid nanocarriers with an unstructured matrix, presenting potentially advantageous nanocarrier systems with marketable opportunities because of reproducible production methodologies and biocompatible lipidic excipients. These (NLCs) are now recognized as a very promising nanocarrier structure for the efficient delivery of drugs via different administration routes. In recent years, several NLC-based gels have been developed and evaluated for topical delivery of many drugs and other therapeutic agents. This review article presents an overview of NLC-based topical gels investigated to deliver drugs via ocular, dermal, and transdermal routes. In addition, the classification, manufacturing, characterizations, advantages, and disadvantages of NLCs are addressed in this article. We also discussed different evaluations of NLC-based topical gels.

Background: Fungal keratitis (mycotic keratitis) is an eye infection in which the cornea is infected by fungi and such fungal keratitis management can be effectively possible by ocular administration of antifungal drugs.

Objective: The main objectives of the present research were to develop and evaluate fluconazoleloaded transfersomal hydrogels for ocular delivery in the effective management of fungal keratitis.

Methods: A 23 factorial design-based approach was used for statistical optimization, where (A) the ratio of lipid to edge activators, (B) the amount of hyaluronic acid (% HA), and (C) the ratio of edge activators (sodium deoxycholate to Span 80) were taken as three factors. The average vesicle diameter (Z, nm) of transfersomes was taken as a response. Further, fluconazole-loaded transfersomes (FTO) were incorporated into 1% Carbopol 940-based hydrogel (OF1) and 2% HMPC K4M-based hydrogel (OF2) containing D-panthenol (5% w/w).

Results: The optimal variable setting for the optimized formulations of FTO was (A) = 9.15, (B) = 0.30%, and (C) = 3.00. FTO exhibited 66.39 nm Z, 0.247 polydispersity index, - 33.10 mV zeta potential, and 65.38 ± 1.77 % DEE, and desirable elasticity. TEM image of FTO demonstrated a unilamellar vesicular structure. The ex vivo ocular permeation of fluconazole from transfersomal hydrogels was sustained over 24 h. All the transfersomal hydrogels showed good bioadhesion and excellent antifungal activity with respect to the zone of inhibition against Candida albicans than Aspergillus fumigates, in vitro. HET-CAM study results demonstrated that both the hydrogels were nonirritant and safe for ocular. Short-term physical stability study suggested the stability of the developed formulation.

Conclusion: The current research demonstrated a new way to enhance the ocular penetration of fluconazole via transfersomal hydrogel formulations for ocular delivery in the effective management of fungal keratitis.