Therapeutic delivery最新文献

Introduction: Sulphasalazine (Sulf) is a class IV compound with low aqueous solubility and low permeability which limit its therapeutic activity. This work aims to apply choline chloride (CC) and choline hydroxide (CH) as a hydrogen bond acceptor with Sulf for the production of Sulf salt.

Materials and method: New compounds were prepared and characterized by XRD, DSC, and FT-IR. Drug solubility was evaluated in different media including pure water, and buffer pH 1.2, 4.5, and 6.8 were evaluated.

Results: The diffractogram pattern of the Sulf-CH shows a smooth and low-intensity diffraction which may indicate amorphization of the drug molecule. The FT-IR spectra confirm participation of the carboxyl group of Sulf in the formation of hydrogen bonding between Sulf and CH through salt formation which helps to enhance drug solubility. Solubility of Sulf-CH significantly increased up to 10,000-folds in pure water. Sulf-CC caused up to 2-folds enhancement in drug solubility.

Conclusion: The difference in the solubility of Sulf-CC and Sulf-CH may suggest that each of these compounds involve different intermolecular interactions which were also confirmed by FT-IR, XRD, and DSC results. This effect can influence drug bioavailability and enhance its therapeutic efficacy.

Oxygen therapeutics hold great potential as alternatives to red blood cell/whole blood transfusions. The development of hemoglobin-based oxygen carriers began in the 1930s, but, regrettably, none have received FDA approval. This review starts with an overview of red blood cell physiology and then focuses on hemoglobin-based oxygen therapeutics (including modified and encapsulated hemoglobin) as well as red blood cell mimetics, particularly regarding their size and shape. The review also addresses the different approaches to hemoglobin-based oxygen carriers.

Aims: This study aimed to develop microparticles of N-phenyl-2,2-dichloroacetamide (PDA), a chloramphenicol derivative with potential antibacterial and anticancer properties, to improve drug release and selectivity while reducing toxicity.

Materials & methods: PDA microparticles were prepared via spray-drying using L-leucine, Trehalose, and Mannitol. The particles were characterized for size, drug release, antibacterial activity, and cytotoxicity against A549 cancer cells and fibroblasts.

Results: PDA formulations exhibited controlled release and enhanced selectivity for cancer cells. S1 showed antibacterial activity against S. aureus. L-leucine formulations had reduced toxicity to normal fibroblasts.

Conclusions: PDA microparticles offer potential as safer, targeted antibacterial and anticancer therapies, providing controlled release and reduced side effects.

Aim: This study focuses on the synthesis and evaluation of innovative gold nanoparticles (AuNps) stabilized by short-chain ferulic acid (FA), specifically 4-hydroxy-3-methoxy-cinnamic acid.

Methods: We analyzed the size and distribution of FA-TSC-AuNps and FA-NaBH4-AuNps, with the reduction kinetics of Au3 + to Au0. The electronic and optical properties of these AuNps were scrutinized using UV-visible, AFM, and FT-IR.

Results: AFM distinctly showcased spherical particles, average diameters of 4 ± 1 nm for FA-TSC-AuNps and 11 ± 1 nm for FA-NaBH4-AuNps systems. In the DPPH assay, the anti-scavenging activity recorded values of: FA at 15.4% ± 0.32, FA-TSC-AuNps at an impressive 86.8% ± 0.32, and FA-NaBH4-AuNps at 61.5% ± 0.22. The ABTS assay yielded results of: FA at 13%, FA-TSC-AuNps at 70.14%, and FA-NaBH4-AuNps at a remarkable 92.8%. Catalytic investigations revealed that both facilitated the swift conversion of p-nitrophenol to p-aminophenol. Additionally successful chemo sensing capabilities were assessed, particularly in relation to ciprofloxacin antibiotic by distinct shift in color signifies the effective detection capability of both sensory systems for the drug. Moreover, with FA-TSC-AuNps exhibiting significant sensitivity toward aluminum.

Conclusion: These nanoparticles suggest promising avenues for drug system modifications and enhancements, highlighting their multifaceted potential in both catalytic and chemo sensing applications.

This review explores the advancements in drug delivery systems that incorporate bile salts since bilosomes that were developed over 20 years ago. Bile salts, recognized for their unique amphiphilic properties, have emerged as versatile agents in enhancing solubility, stability, and bioavailability of various therapeutics. We discuss the innovative formulations developed, including micelles, liposomes, and nanoparticles, that leverage bile salts to facilitate targeted and sustained release. The review also highlights the mechanisms by which bile salts improve drug absorption, particularly for hydrophobic compounds, and examines the evolving regulatory landscape surrounding these systems. Furthermore, we address challenges faced in clinical translation and future directions for research, emphasizing the potential of bile salt-based systems in personalized medicine. Our evaluation highlights the significant role of bile salts in advancing drug delivery technologies and their promise for improving therapeutic outcomes.

Aims: This study aimed to evaluate the potential of Eryngium maritimum L. (EM) callus media filtrate (ECMF) for enhanced skin delivery through multilayered liposomes (MLs).

Materials & methods: ECMF was applied to human skin cells to assess its antioxidant, anti-inflammatory, and skin barrier-enhancing properties. ECMF was encapsulated in MLs to enhance delivery efficiency, creating a formulation called Cellbiome. Clinical trials involving human participants were conducted to compare its effects with traditional formulations, assessing parameters such as skin density, hydration, elasticity, and wrinkle reduction.

Results: Cellbiome significantly improved skin density and moisturization, outperforming conventional formulations. ML encapsulation facilitated deeper penetration of active ingredients beyond the stratum corneum, leading to synchronized improvements in multiple skin parameters, including elasticity, wrinkle reduction, and overall skin health. Transcriptomic and metabolomic analyses further confirmed ECMF's bioactivity and its role in skin improvement.

Conclusions: ML-based formulations, such as Cellbiome, offer superior efficacy in skincare applications compared to conventional methods. This study underscores the importance of advanced delivery technologies in cosmetics and highlights the need for further research to optimize the benefits of natural extracts like EM for human skin, potentially advancing dermatological and cosmeceutical applications.

Aim: This research aims to develop nanostructured lipid carriers containing Lurasidone hydrochloride (LH) with Quality by Design (QbD) methodology to enhance its bioavailability, given LH's low water solubility (0.224 mg/ml) and bioavailability (9-19%).

Material and methods: The optimized LH-NLC formulation contains Glyceryl monostearate (GMS) as solid lipid, Caproyl 90 as liquid lipid and co-surfactant, and Tween 80 as surfactant. The hot emulsification method was used to formulate the LH-NLC using a three-factor, three-level Box-Behnken design (BBD)for ascertaining functional relationships between particle size and entrapment efficiency (EE). Particle size, polydispersity index (PDI), zeta potential, surface morphology, percentage EE, and in vitro and ex-vivo release were assessed. Wistar rats were used to estimate plasma drug concentration after LH-NLC administration.

Results: The developed formulation exhibited a particle size of 190.98 ± 4.72 nm, zeta potential of + 17.47 mV, and encapsulation efficiency of 94 ± 1.26% w/w. LH-NLCs showed a drug release rate of 95.37% within 24 hours. Intranasal administration of LH-NLCs resulted in 5.16 times higher bioavailability compared to intranasally administered lurasidone.

Conclusion: The study successfully applied QbD methodology to develop NLCs for LH with enhanced bioavailability, demonstrating improved drug entrapment and delivery efficacy for treating psychosis.

Gliomas are prominent and frequent primary malignant brain tumors, with a generally poor prognosis. Current treatment involves radiation, surgery and chemotherapy. Exosomes are nanoscale extracellular vesicles released by cells that enable biological molecule movement and encourage intercellular communication in the tumor microenvironment. This contributes to glioma development, radiation resistance, and overcomes chemotherapy. Exosome functional and structural properties are essential for understanding cancer molecular mechanisms. They can also treat invasive tumors like glioblastomas and serve as diagnostic markers. Recent research depicted exosomes' prominent role in cancer cell maintenance, intercellular signaling, and microenvironment modification. Exosomes hold nucleic acids, proteins, lipids, mRNAs, lncRNAs, miRNAs, and immunological regulatory molecules depending on the origin of the cell. This paper reviews exosomes, their role in glioma etiology, and perspective diagnostic and therapeutic uses.