Therapeutic delivery最新文献

November 2025 saw the approval of a number of products which employ a variety of delivery technologies including Johnson and Johnson's DARZALEX FASPRO (with Haloyzyme's ENHAZE), Merck's KEYTRUDA QLEX, and Regeneron's EYLEA HD. It was also a busy month for acquisitions with Halozyme completing the acquisition of Elektrofi which gives it access to the microparticulate technology Hypercon. Halozyme also announced a collaboration with the Dutch company Merus, for the development of a subcutaneous formulation of petosemtamab. Positive clinical trial data was announced for a number of companies including EyePoint, Tiziana, Nasus, and Tonix.

Aim: Lutein exhibits poor aqueous solubility, chemical instability, and low bioavailability following oral administration, which restricts its therapeutic use in Alzheimer's disease (AD). Hence, a lutein-laden liposomal in situ gel was formulated to enhance bioavailability and brain targeting via nasal delivery.

Method: Lutein-laden liposomes were fabricated using an ethanol injection method and studied for various parameters.

Result and conclusions: The formulated lutein-laden liposomes showed a particle size, polydispersity index, and encapsulation efficiency of 71.8 $\pm$ 6.4 nm, 0.327 $\pm$ 0.007, and 95.59 $\pm$ 3.03%, respectively. The permeation studies on goat nasal mucosa revealed drug permeation from the lutein-laden liposomal in situ gel and fivefold higher permeation than the lutein solution-based in situ gel. The drug targeting efficiency of the developed formulation was 372.80%. The pharmacokinetic study of the developed formulation administered via the nasal route showed a twofold higher C_max and a 1.7-fold higher AUC than the drug suspension administered via the oral route. The histopathological analysis indicated that the developed formulation was safe. Thus, intranasal delivery of lutein could surpass poor oral bioavailability and be studied for managing AD and its symptoms using an intranasal delivery-based brain-targeted approach.

Aims: Carboxymethyl cellulose (CMC) and xanthan gum (XG) are promising polysaccharides for hydrogel fabrication in 3D bioprinting and controlled drug delivery. Due to the complex polymer structure of these hydrogels and their ability to swell, a prolonged release of drugs is possible. This study aimed to evaluate different ratios of CMC and XG for fabrication of composite hydrogels with extrusion-based 3D printing.

Materials and methods: The printability, filament fusion, and post-printing shape retention of hydrogels containing various ratios of CMC and XG (0.5:2, 1:1, 1:2, 2:1) as well as swelling, degradation, and release of vancomycin hydrochloride were analyzed. The viability of Vero cells was also assessed at 1:2 and 2:1 ratio.

Results: Using a ratio of CMC and XG of 1:2 or 2:1 was critical for achieving optimal printability, characterized by the improved printing resolution and enhanced shape retention. Consistent vancomycin hydrochloride release with the prolonged antimicrobial activity over 9 days was evident for 1:2 ratio. Viability of Vero cells was lower for both 1:2 and 2:1 ratio compared to control and in 1:2 alone.

Conclusion: Consistent drug release and appropriate printability of these hydrogels, particularly at the 1:2 ratio, warrant their further investigation and improvement.

Introduction: Simvastatin (SIM), a commonly used lipid-lowering drug, exhibits pleiotropic effects with potential for dermatological applications. This study aimed to analyze the in vitro release and rheological properties of SIM from three extemporaneously prepared topical formulations.

Methods: Formulations were prepared from commercially available SIM tablets. A structured risk assessment confirmed the low-risk profile of these preparations. SIM content and dissolution profiles were evaluated using high-performance liquid chromatography (HPLC). In vitro release testing was conducted using vertical diffusion cells fabricated by using fused deposition modeling (FDM) technology of 3D printing with polylactic acid (PLA).

Results: The cream demonstrated the most favorable release characteristics, while the ointment exhibited the greatest resistance to rheological alteration following incorporation of powdered tablets. The 3D-printed diffusion cells ensured reproducibility and adaptability for topical product evaluation. Thixotropy was observed in all tested formulations. Overall, elastic behavior dominated, and the effect of tablet powder on viscosity and structure varied depending on the formulation base.

Conclusion: Formulation type significantly influenced SIM release and rheological properties. The findings highlight the utility of low-cost 3D-printed diffusion systems in preclinical topical research and support further translational development of repurposed SIM formulations for skin-related indications.

While ultrasound-based medical imaging is widely used in clinics, ultrasound-triggered drug delivery represents an emerging modality that takes advantage of the high tissue penetrability, general safety, and high clinical accessibility of ultrasound to solve key challenges around localized drug delivery. In this review, we analyze emerging trends in the design of drug delivery vehicles activated using different ultrasound effects ranging from cavitation, mechanical stimulation, localized heating, reactive oxygen species generation, localized gas generation, and/or penetration enhancement. In particular, we focus on vehicle designs that enable delayed burst release, sustained release, and pulsatile on-off release of drugs locally at the targeted ultrasound site, each of which has direct applications for treating specific diseases. Vehicles in which ultrasound-mediated drug release kinetics control is synergistically coupled with other therapeutic benefits of ultrasound are highlighted. Finally, we discuss key barriers to the practical translation of ultrasound-triggered drug delivery vehicles into the clinic, aiming to motivate the design of scalable and reproducible ultrasound-triggered drug delivery vehicles that can have real-world patient impact.

The growing interest in naturally derived compounds as therapeutic agents has led to an ongoing search for innovative delivery systems that can improve their bioavailability and therapeutic efficacy. Nanoemulgels, a hybrid system that combines the benefits of nanoemulsions and hydrogels, offer a promising approach to enhance the delivery and efficacy of these bioactive compounds. This review presents the pharmaceutical applications of nanoemulgels containing naturally derived compounds, along with the challenges and future perspectives. The review explores the interaction between nanoemulgels and distinct types of natural compounds, highlighting how the formulation can be adjusted to maximize the therapeutic effects of each class of substance. In particular, the challenges and strategies for incorporating unstable compounds into nanoemulgels, ensuring their stability and efficacy over time, are discussed. Nanoemulgels represent a promising and versatile platform for enhancing the therapeutic efficacy of naturally derived compounds. By improving the bioavailability and controlled release profiles of these compounds, nanoemulgels can significantly enhance their therapeutic effects in a variety of clinical settings. The combination of biocompatibility, biodegradability, and versatility makes nanoemulgels an exciting area for future research, particularly in personalized medicine and natural product-based therapies.

Objective: To circumvent the blood-brain barrier (BBB), spanlastics was utilized as the drug delivery carrier. The present research focused on development and evaluation of spanlastics via intranasal route to overcome bioavailability issue of Midazolam (MZ). To reduce the oxidative stress in brain during seizures, Coenzyme Q10 (CQ) was used in this study for management of status epilepticus.

Methods: Midazolam-Coenzyme Q10 loaded spanlastics (MZ-CQ-SPL) were formulated by ethanol injection method followed by optimization with Central composite rotatable design (CCRD). They were then evaluated by performing characterization parameters, in vitro and ex vivo analysis, followed by pharmacodynamic and histopathological studies.

Results: Spanlastics demonstrated particle size of 157 nm with high entrapment efficiency (MZ: 80.80 ± 1.66%; CQ: 76.98 ± 1.92%). In vitro release showed sustained release profile (MZ: 91.36 ± 1.26%; CQ: 84.91 ± 1.37%) in 24 h. Ex vivo permeation showed 1.95- and 2.82-times enhanced flux across the nasal mucosa for MZ and CQ, respectively. Pharmacodynamic study revealed enhanced antiepileptic potential of MZ-CQ-SPL in delaying seizure onset along with reducing the severity of seizures.

Conclusion: Outcomes concluded the potential of spanlastics in enhancing the bioavailability and therapeutic applicability of MZ and CQ in combination therapy for effective management of seizures.

HIV-associated neurocognitive disorders (HAND) persist in a significant proportion of HIV patients, despite combination antiretroviral therapy (cART), due to limited drug penetration across the blood-brain barrier (BBB) and the establishment of viral reservoirs within the central nervous system (CNS). Intranasal drug delivery offers a promising, noninvasive route to bypass the BBB and directly target the brain through olfactory and trigeminal pathways. This review explores the pharmacology of antiretroviral drugs, the challenges they face in CNS delivery, and the advantages of intranasal administration for treating NeuroAIDS. We examine physicochemical properties influencing BBB penetration and the mechanisms of nose-to-brain transport, along with their benefits and challenges. The review further evaluates the use of polymeric and lipid-based nanocarrier systems that improve drug stability, nasal residence time, and neuronal transport. Key anatomical considerations for targeting the olfactory region and design parameters for specialized intranasal delivery devices are also discussed. Despite anatomical and physiological challenges, advancements in nanotechnology and device engineering are enhancing CNS drug delivery efficiency. Combining antiretroviral-loaded nanocarriers with targeted nasal delivery devices represents a compelling strategy to improve therapeutic outcomes for HAND. This integrative approach holds significant potential to overcome CNS viral reservoirs, reduce neurocognitive impairment, and advance the eradication of NeuroAIDS.

Introduction: Wound dressings help to prevent the wound from being infected and allow gaseous exchange, along with absorbing excessive wound exudates. Open wounds are very prone to bacterial infection, mostly Staphylococcus aureus may hinder the healing rate. Therefore, a fast, safe, effective, biodegradable antimicrobial wound dressing material needs to be developed. In this research, a basic fibroblast growth factor and mupirocin co-loaded biodegradable polymeric sponge was developed and evaluated for wound dressing applications.

Methods: An Antimicrobial gelatin-chitosan sponge was prepared by the surfactant foaming method. Different combinations were prepared and evaluated for water uptake, digestibility, porosity, folding endurance, morphology, FT-IR analysis, drug-loading, entrapment efficiency, in-vitro drug release, antimicrobial study, in-vivo study using rat excision model, along with histological analysis.

Results: The Developed sponge was found with satisfactory water uptake capacity (76.96 ± 0.79%), porosity (71.64 ± 0.7), and folding endurance (251.33 ± 4.33%), and was completely digested. Microscopy confirms the internal porous structure. Drug loading and entrapment efficiency of the final formulation were found to be 1.859 ± 0.024% and 92.95 ± 1.09%, respectively. The formulation releases 88.018 ± 3.12% mupirocin in 5 hours and best fitted in the Korsmeyer-Peppas kinetic model with a non-Fickian transport mechanism. Antimicrobial studies show a zone of inhibition of 37±2.65 mm. The wound healing study and histological studies of the formulation showed accelerated wound contraction and healing efficacy.