Current drug delivery最新文献

Introduction: Poly(methyl vinyl ether co-maleic acid) (PMVE/MA) hydrogel microneedles (HMN) are investigated for transdermal delivery of macromolecular drugs owing to their biocompatibility and super-swelling properties. However, the drug delivery efficacy reduces with increasing molecular weight due to the entrapment within the HMN matrices. Furthermore, integrating external drug reservoirs extends the drug diffusion path and reduces the efficiency of drug permeation.

Methods: A direct drug loading approach in the HMN matrix was introduced in this work following a pH modification step. The effect of pH modification on the physicochemical properties of HMN was studied. Then, bovine serum albumin (BSA), a model protein, was loaded into the pH-modified HMN, and the morphological changes in HMN and protein stability were also assessed. Finally, the efficacy of BSA-loaded HMN in the transdermal delivery was evaluated ex vivo.

Results: A significant increase in swelling was recorded following the pH modification of HMN (p < 0.001). The structure of pH-modified hydrogel was highly porous, and ATR-FTIR spectra indicated a shift in the carboxylic peak. The secondary structure of BSA loaded in the pH-modified HMN was also preserved. The BSA-loaded HMN mediated a sustained ex-vivo drug release with a cumulative release of 64.70% (3.88 mg) in 24 h.

Conclusion: Hence, the model drug-incorporated PMVE/MA HMN system shows potential for sustainable transdermal delivery of proteins.

Background: Hot-melt Pressure-sensitive Adhesives (HMPSA) are eco-friendly pressuresensitive adhesives, with the potential of being used as substrates for transdermal patches. However, due to the low hydrophilicity of HMPSA, the application is limited in the field of Traditional Chinese Medicine (TCM) plasters.

Methods: Three modified HMPSA were prepared with acrylic resin EPO, acrylic resin RL100, and Polyvinylpyrrolidone (PVP) as the modifying materials. The physical compatibility between HMPSA and the modifying materials was investigated through in vitro release performance, viscosity, softening point, cohesion, and fluidity, so as to determine the most effective modifying material. The impact of the modified HMPSA on the release properties of different TCM ingredients was elucidated by the performance of water absorption and contact angle behavior.

Results: With the addition of the modifying materials, both the viscosity and the softening point of HMPSA were improved, with the flowability reduced and the cohesion maintained. The morphological and structural changes reflected the physical compatibility between HMPSA and the three modifying materials. According to the results of in vitro release experiments, PVP effectively improved the release performance of paeoniflorin, ephedrine hydrochloride, and cinnamaldehyde in HMPSA, with no significant impact on the release performance of eugenol. The changes in the drug release performance of HMPSA may be attributed to the improved hydrophilicity of HMPSA after physical modification.

Conclusion: The compatibility and the drug release performance of HMPSA were effectively enhanced after the addition of the modifying materials by the physical blending technique. Among the three modifying materials, PVP has been found to be an ideal modifying material for HMPSA in the field of TCM plasters due to its effects on drug release performance.

Prokinetic agents are drugs used to enhance gastrointestinal motility and treat disorders such as Gastroesophageal Reflux Disease (GERD) and gastroparesis. pH-dependent release systems offer targeted drug delivery, allowing prokinetic agents to be released specifically in desired regions of the gastrointestinal tract. This optimizes drug efficacy and minimizes systemic side effects. Gastroretentive formulations enable sustained drug release, which is particularly beneficial in conditions requiring prolonged gastric residence time, such as gastroparesis. Nanoparticles have emerged as promising carriers for improving prokinetic agent delivery and enhancing drug stability, solubility, and absorption. These nano-systems protect drugs from degradation, leading to improved bioavailability and controlled drug release. Furthermore, incorporating mucoadhesive technologies promotes prolonged drug-mucosa interactions, facilitating enhanced drug absorption and reducing dosing frequency. These recent advancements have the potential to revolutionize the oral drug delivery of prokinetic agents, offering improved therapeutic outcomes, enhanced patient compliance, and reduced side effects. However, scalability, biocompatibility, and safety challenges warrant further investigation and validation through preclinical and clinical studies. This review highlights recent advances in oral drug delivery systems for prokinetic agents, focusing on innovative approaches such as pH-dependent release, gastroretentive formulations, nanoparticles, and mucoadhesive technologies. In conclusion, integrating advanced oral drug delivery systems for prokinetic agents presents a promising avenue for managing gastrointestinal disorders. Continued research and collaboration among academia, industry, and healthcare professionals are crucial to unlocking the full potential of these innovations and ultimately translating them into clinically effective treatments for patients.

Due to the blood-brain barrier (BBB) and issues with oral and other traditional routes of administration, psychiatric disorders present significant challenges in getting therapeutics into the brain. The nose-to-brain pathway, also known as intranasal delivery, has shown promise in overcoming these barriers since it targets the brain directly and bypasses the BBB. This review explores nanocarriers' potential for intranasal delivery of therapeutics in the treatment of psychiatric disorders. Nanocarriers, such as polymeric nanoparticles, liposomes, and nanoemulsions, offer unique advantages for enhancing the delivery of various therapeutic agents to the brain via the intranasal route. The methodology involved conducting preliminary searches on databases such as PubMed, ScienceDirect, Web of Science, and Google Scholar using keywords related to "psychiatric disorders, intranasal delivery, nose-to-brain drug delivery, and nano formulations for intranasal delivery." This review highlights the advantages of the intranasal drug delivery pathway as a non-invasive, reliable, and efficient method for targeting the brain by bypassing the BBB. Furthermore, it discusses the application of various novel nanocarrier-based formulations, including nanoparticles, in-situ gels, nanoemulsions, hydrogels, and liposomes, for the effective intranasal delivery of therapeutics in the treatment of psychiatric conditions such as mood and anxiety disorders schizophrenia, and other illnesses.

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.