Drug Delivery Systems Research Articles

Design and In Vitro Evaluation of Fluorescent MOF-Core CaCO₃-PEI-FA Shell Nanoparticles for Targeted Therapy of Laryngeal Cancer Cells.

Laryngeal cancer, a common malignant respiratory tumor, is primarily treated through surgery. However, challenges such as recurrence, metastasis, and drug resistance persist. In recent years, multifunctional drug delivery systems (DDS) based on nanoparticles have shown great potential in improving drug loading and release. We developed a biocompatible core-shell nanoparticle system with a zinc-based metal-organic framework (MOF) as the core, named CP1. The shell, composed of polyethyleneimine (PEI), folic acid, and calcium carbonate, forms a composite called CaCO3-PEI-FA. This system enhances biocompatibility and increases the efficacy of biomedical applications. Encapsulating CP1 within the CaCO3-PEI-FA shell allows for the targeted delivery of the anticancer drug doxorubicin (DOX) to laryngeal cancer cells (Hep-2), resulting in the CaCO3-PEI-FA@CP1@DOX system. The CaCO3-PEI-FA composite exhibits strong fluorescence with a peak around 350nm, confirming successful synthesis and demonstrating its potential as a bioimaging probe. Importantly, the nanoparticle system without DOX showed low toxicity to normal human skin fibroblasts (HSF). In vitro cytology experiments revealed a 38% inhibition rate of Hep-2 cells after 24h, highlighting the nanocomposite's significant potential in inhibiting laryngeal cancer cell proliferation and inducing apoptosis, underscoring its promise in targeted laryngeal cancer therapy.

Active CNS delivery of oxycodone in healthy and endotoxemic pigs

BackgroundThe primary objective of this study was to advance our understanding of active drug uptake at brain barriers in higher species than rodents, by examining oxycodone brain concentrations in pigs.MethodsThis was investigated by a microdialysis study in healthy and endotoxemic conditions to increase the understanding of inter-species translation of putative proton-coupled organic cation (H+/OC) antiporter-mediated central nervous system (CNS) drug delivery in health and pathology, and facilitate the extrapolation to humans for improved CNS drug treatment in patients. Additionally, we sought to evaluate the efficacy of lumbar cerebrospinal fluid (CSF) exposure readout as a proxy for brain unbound interstitial fluid (ISF) concentrations. By simultaneously monitoring unbound concentrations in blood, the frontal cortical area, the lateral ventricle (LV), and the lumbar intrathecal space in healthy and lipopolysaccharide (LPS)-induced inflammation states within the same animal, we achieved exceptional spatiotemporal resolution in mapping oxycodone transport across CNS barriers.ResultsOur findings provide novel evidence of higher unbound oxycodone concentrations in brain ISF compared to blood, yielding an unbound brain-to-plasma concentration ratio (Kp,uu,brain) of 2.5. This supports the hypothesis of the presence of the H+/OC antiporter system at the blood–brain barrier (BBB) in pigs. Despite significant physiological changes, reflected in pig Sequential Organ Failure Assessment, pSOFA scores, oxycodone blood concentrations and its active net uptake across the BBB remained nearly unchanged during three hours of i.v. infusion of 4 µg/kg/h LPS from Escherichia coli (O111:B4). Mean Kp,uu,LV values indicated active uptake also at the blood-CSF barrier in healthy and endotoxemic pigs. Lumbar CSF concentrations showed minimal inter-individual variability during the experiment, with a mean Kp,uu,lumbarCSF of 1.5. LPS challenge caused a slight decrease in Kp,uu,LV, while Kp,uu,lumbarCSF remained unaffected.ConclusionsThis study enhances our understanding of oxycodone pharmacokinetics and CNS drug delivery in both healthy and inflamed conditions, providing crucial insights for translating these findings to clinical settings.

Colistin–niclosamide-loaded nanoemulsions and nanoemulsion gels for effective therapy of colistin-resistant Salmonella infections

Colistin (COL) is regarded as a last-resort treatment for infections by multidrug-resistant (MDR) Gram-negative bacteria. The emergence of colistin-resistant Enterobacterales poses a significant global public health concern. Our study discovered that niclosamide (NIC) reverses COL resistance in Salmonella via a checkerboard assay. However, poor solubility and bioavailability of NIC pose challenges. In this study, we prepared a self-nanoemulsifying drug delivery system (SNEDDS) co-encapsulating NIC and COL. We characterized the physicochemical properties of the resulting colistin–niclosamide-loaded nanoemulsions (COL/NIC-NEs) and colistin–niclosamide-loaded nanoemulsion gels (COL/NIC-NEGs), assessing their antibacterial efficacy in vitro and in vivo. The COL/NIC-NEs exhibited a droplet size of 19.86 nm with a zeta potential of −1.25 mV. COL/NIC-NEs have excellent stability, significantly enhancing the solubility of NIC while also demonstrating a pronounced sustained-release effect. Antimicrobial assays revealed that the MIC of COL in COL/NIC-NEs was reduced by 16–128 times compared to free COL. Killing kinetics and scanning electron microscopy confirmed enhanced antibacterial activity. Antibacterial mechanism studies reveal that the COL/NIC-NEs and COL/NIC-NEGs could enhance the bactericidal activity by damaging cell membranes, disrupting proton motive force (PMF), inhibiting multidrug efflux pump, and promoting oxidative damage. The therapeutic efficacy of the COL/NIC-NEs and COL/NIC-NEGs is further demonstrated in mouse intraperitoneal infection models with COL-resistant Salmonella. To sum up, COL/NIC-NEs and COL/NIC-NEGs are a potentially effective strategies promising against COL-resistant Salmonella infections.

Comparative evaluation of analgesic efficacy of buprenorphine transdermal patch and fentanyl transdermal patch in the management of postoperative pain after lower limb surgery

Background: Postoperative pain represents a significant medical issue that needs immediate attention. Despite advancements in pain management, managing postoperative pain remains challenging. Transdermal drug delivery systems (TDDS) offers a straightforward, reliable, non-invasive, and patient-friendly approach for alleviating post-surgical pain. Hence, this study was planned to evaluate the analgesic efficacy of buprenorphine and fentanyl transdermal patch in the management of post-operative pain after lower limb surgery. Methods: In this prospective, randomised study, 82 adult patients of either sex undergoing elective lower limb surgery were randomly allocated into two groups- Group A (Transdermal Buprenorphine 20 mg patch) and Group B (Transdermal Fentanyl 50 mcg patch). Postoperative pain was assessed by 10-point Visual Analogue Scale (VAS) every 6 hours following surgery on the first day and then daily for next 4 days. All patients were also monitored for total rescue analgesic requirement, drug-related adverse effect and haemodynamic status. Statistical analysis was carried out using student t-test and Chi-square test. A p-value <0.05 was considered significant. Results: The mean pain intensity scores were found to be significantly different (p<0.0001) between the two groups, with VAS scores consistently lower in Buprenorphine group as compared to Fentanyl group. Also, Buprenorphine group had the lowest demand for rescue analgesic, with 58.5% of patients requiring two administrations and 36.6% needing only one. Patients belonging to Fentanyl group exhibited higher occurrence of nausea (46.3%), vomiting (46.3%) and pruritus (31.7%). Conclusions: Our study concludes that transdermal patch of buprenorphine demonstrates superior efficacy and safety profile as compared to fentanyl patch for post-operative pain management in lower limb surgeries.

Drug Delivery Based on Nanoparticulate Systems

The administration route of an active ingredient and the materials used to deliver it are as important as the synthesis of that active ingredient. For the treatment to be effective, the active ingredient must be present in the right amount and in the right place at the right time. Therefore, researchers have been studying a wide variety of drug delivery systems, taking into account the route of administration of the drug, its half-life, and its effective and toxic amounts. Because of its numerous benefits, nanotechnology has attracted attention in pharmaceutical research as well as many other fields. Nanoparticles have the potential to disperse hydrophobic drugs in an aqueous solution, deliver drugs to the targeted site, and thus selectively direct therapeutic agents such as antineoplastic drugs. This study provides a detailed discussion of the many inorganic, polymeric, and lipid-based nanoparticulate systems designed for drug delivery.

Hydrogel encapsulating gold nanoparticles for targeted delivery of nitroglycerin to reduce post-cardiac dysfunction inflammation by inhibiting the Wnt/β-catenin signaling pathway.

The discovery of nitric oxide's role in biological processes like platelet function, vasodilation, cell permeability, and inflammation has advanced our understanding of organic nitrate therapy's hemodynamic and nonhemodynamic effects. Short-term use of organic nitrates prevents left ventricular enlargement and infarct expansion. However, information on their long-term impact on LV remodeling in post-acute cardiac dysfunction patients is limited. In this study, we utilized an innovative active hydrogel with gelatin (Gel)/polyethylene glycol (PEG)/polylactic acid (PLA) encapsulating gold nanoparticles (AuNPs)-based drug delivery system for the sustained release of nitroglycerin (NTG). Gel/PEG/PLA/NTG/AuNPs hydrogel-based system is a non-transplant surgical method that can adhere to the surface of the heart and deliver the drug directly to the epicardium. Cardiac dysfunction was induced by ligating the left anterior descending coronary artery. Echocardiograms were used to study the pre- and post-operative hemodynamics. Hematoxylin and eosin (H&E) and Masson's trichrome stain (MTS) stainingrevealed that the acute myocardial infarction (AMI) rats' group had irregularly shaped fibers and a lack of transverse striations, whereas Gel/PEG/PLA/NTG/AuNPs hydrogel group showed significant improvement. Rats in the Gel/PEG/PLA hydrogel group demonstrated marked vasodilation, compared to the AMI group. Mechanistically, we determined that hydrogel disrupts the initiation of post-cardiac dysfunction via inhibiting Wnt/β-catenin transcriptional activation. Hence, the Gel/PEG/PLA/NTG/AuNPs hydrogel group effectively protected against ischemic injury and inflammation in AMI, demonstrating a novel method for treating acute cardiac dysfunction.

Effect of Solvent and Cholesterol on Liposome Production by the Reverse-Phase Evaporation (RPE) Method.

Liposomal drug delivery is a promising approach for delivering therapeutics effectively. While most liposomes are designed to be nanometer-sized for efficient cellular uptake, micron-sized liposomes are gaining interest due to their larger drug-loading capacity. When combined with macroscale structures, such as implants and hydrogels, they offer prolonged therapeutic delivery. This study investigates how solvents affect the production of micron-sized liposomes, with or without cholesterol, using the reverse-phase evaporation (RPE) method. Although the RPE method is established for producing micron-sized liposomes, the influence of solvents on liposome size and uniformity is not well understood. The study explores whether controlling the size of inverse micelles, an intermediate product, through the use of different organic solvents affects the final liposome size. Three solvents─diethyl ether, methanol, and acetone─were tested for their effect on the formation of inverse micelles and liposomes and their sizes. Results showed that without cholesterol, diethyl ether produced uniform inverse micelles, leading to mostly nanosized liposomes. Methanol and acetone resulted in phase separation, preventing uniform liposome formation, although some micron-sized liposomes appeared. The acetone sample yielded mostly oil droplets. The results showed that forming inverse micelles lead to nanosized liposomes. With cholesterol, phase separation was dominant in methanol, but micron-sized liposomes still formed. Across all cases, cholesterol reduced the liposome size. The findings reveal that inverse micelles are not always reliable predictors of the final liposome size and that the RPE method is highly sensitive to solvent polarity and lipid-solvent interactions. Overall, the findings of this study provide valuable insights into how the choice of solvent and lipid composition can influence the production of liposomes via the RPE method. These insights are critical for optimizing liposome production and influencing future designs of liposomal drug delivery systems.

Research Progress on Peptide Drugs for Type 2 Diabetes and the Possibility of Oral Administration

Diabetes is a global disease that can lead to a range of complications. Currently, the treatment of type 2 diabetes focuses on oral hypoglycemic drugs and insulin analogues. Studies have shown that drugs such as oral metformin are useful in the treatment of diabetes but can limit the liver’s ability to release sugar. The development of glucose-lowering peptides has provided new options for the treatment of type 2 diabetes. Peptide drugs have low oral utilization due to their easy degradation, short half-life, and difficulty passing through the intestinal mucosa. Therefore, improving the oral utilization of peptide drugs remains an urgent problem. This paper reviews the research progress of peptide drugs in the treatment of diabetes mellitus and proposes that different types of nano-formulation carriers, such as liposomes, self-emulsifying drug delivery systems, and polymer particles, should be combined with peptide drugs for oral administration to improve their absorption in the gastrointestinal tract.

Choline chloride-Urea based deep eutectic Solvent: Characterization, interfacial behavior and Synergism in binary (surfactant) systems

The paper focusses on the synthesis and characterization of choline chloride: urea (molar ratio 1:2) DES. The influence of the varying DES concentration on the surface and interfacial behavior of low-concentration commercial surfactant (cetyl trimethyl ammonium bromide) was examined. The incorporation of DES into the surfactant solution resulted in an augmentation of electrophoretic mobility and absolute zeta potential values, indicative of enhanced surfactant adsorption at the interface. Sessile drop measurements demonstrated the capacity of binary mixture to modify the wettability of sandstone from intermediate-wet state to water-wet condition. In summary, physicochemical evaluation revealed the capability of DES to augment the self-assembly and wetting behavior of surfactant at low concentrations (below critical micelle concentration). The observed phenomenon in these solvents primarily finds utility in nanoscience, drug delivery systems, colloids, catalysis, and applications in many other fields.

Multilayer Nanocarrier for the Codelivery of Interferons: A Promising Strategy for Biocompatible and Long-Acting Antiviral Treatment

Background: Interferons (IFNs) are cytokines involved in the immune response with a synergistic regulatory effect on the immune response. They are therapeutics for various viral and proliferative conditions, with proven safety and efficacy. Their clinical application is challenging due to the molecules’ size, degradation, and pharmacokinetics. We are working on new drug delivery systems that provide adequate therapeutic concentrations for these cytokines and prolong their half-life in the circulation, such as nanoformulations. Methods: Through nanoencapsulation using electrospray technology and biocompatible and biodegradable polymers, we are developing a controlled release system based on nanoparticles for viral infections of the respiratory tract. Results: We developed a controlled release system for viral respiratory tract infections. A prototype nanoparticle with a core was created, which hydrolyzed the polyvinylpyrrolidone (PVP) shell , releasing the active ingredients interferon-alpha (IFN-α) and interferon-gamma (IFN-γ). The chitosan (QS) core degraded slowly, with a controlled release of IFN-α. The primary and rapid effect of the interferon combination ensured an antiviral and immunoregulatory response from day one, induced by IFN-α and enhanced by IFN-γ. The multilayer design demonstrated an optimal toxicity profile. Conclusions: This formulation is an inhaled dry powder intended for the non-invasive intranasal route. The product does not require a cold chain and has the potential for self-administration in the face of emerging viral infections. This novel drug has applications in multiple infectious, oncological, and autoimmune conditions, and further development is proposed for its therapeutic potential. This prototype would ensure greater bioavailability, controlled release, fewer adverse effects, and robust biological action through the simultaneous action of both molecules.

Study of Magnetic Hydrogel 4D Printability and Smart Self‐Folding Structure

4D printing technology offers the potential to create smart structures that respond to external stimuli. This study focuses on a novel magnetic hydrogel with promising applications in 4D printing, particularly for medical devices such as guidewire robots, drug delivery systems, and vascular stents. Magnetic‐responsive hydrogels suitable for 4D printing are scarce, and their complex rheological properties pose challenges for printing. The study investigates these properties and optimizes them through adjustments in ink composition and the application of an external magnetic field, improving printability. Using the direct writing (DLP) method, which allows magnetic programming of individual strands, the study achieves greater flexibility compared to the traditional SLA method. Optimized printing parameters and material ratios produced high‐quality single strands, grids, and sheet‐like structures, demonstrating responsiveness to varying magnetic fields. Results confirm that DLP can be effectively applied to hydrogel 4D printing, achieving flexible structures with tunable mechanical properties. Additionally, magnetic‐responsive, self‐folding hydrogel structures were created, with a response speed of 180 ms under a magnetic field. This research establishes a foundation for magnetic hydrogel 4D printing and offers insights for the development of future smart medical devices.

Cyclophosphamide: Lyo to Liquid – A Comprehensive Review

Cyclophosphamide has been a key chemotherapeutic and immunosuppressive agent for decades. Its development, from lyophilized powder to sterile liquid formulations, represents significant progress in improving drug stability, ease of administration, and patient safety. Initially approved as a lyophilized powder in 1959, Cyclophosphamide provided extended shelf life but required reconstitution before use, posing challenges such as contamination risk and preparation errors. Advances in formulation led to the development of sterile liquid forms, which eliminate the need for reconstitution, offering more convenience and minimizing handling risks. These liquid formulations incorporate stabilizing agents to maintain drug integrity and ensure bioequivalence with the lyophilized form. The review highlights key regulatory milestones, including the first liquid formulation approvals in 2018 and 2020, and discusses the patents that contributed to these innovations. Furthermore, it explores future perspectives, such as improving bioavailability, enhancing patient compliance, and incorporating uroprotective agents directly into the formulation. These advancements are critical for maintaining Cyclophosphamide’s role in oncology and ensuring it remains an effective treatment option for cancer patients. Key Words: Cyclophosphamide, Lyophilized formulation, Sterile liquid formulation, Chemotherapy, Drug stability, Drug delivery systems

Adhesive lipophilic gels delivering rapamycin prevent oral leukoplakia from malignant transformation

Oral leukoplakia (OLK) is the most emblematic oral potentially malignant disorder that may precede the diagnosis of oral squamous cell carcinoma (OSCC) and has an overall malignant transformation rate of 9.8 %. Early intervention is crucial to reduce the malignant transformation rate from OLK to OSCC but the lack of effective local pharmaceutical preparations poses a challenge to clinical management. Rapamycin is speculated to prevent OLK from carcinogenesis and its inherent lipophilicity facilitates its penetration into stratum corneum. Nevertheless, hydrophilic hydrogels frequently encounter challenges when attempting to deliver lipophilic drugs. Furthermore, the oral cavity presents a complex environment defined by oral motor functions, saliva secretion cycles, dynamic fluctuations, and protective barriers comprising mucus and lipid layers. Consequently, addressing issues of muco-penetration and muco-adhesion is imperative for developing an effective drug delivery system aiming at delivering rapamycin to target oral potentially malignant disorders.Here, a dual-function hydrogel drug delivery system integrating adhesion and lipophilicity was successfully developed based on polyvinyl alcohol (PVA) and dioleoyl phosphatidylglycerol (DOPG) via dynamic boronic ester bonds. Rheological experiments based on orthogonal design revealed that PVA-DOPG hydrogels exhibited ideal adhesive strength (around 6 kPa) and could adhere to various surfaces in both dry and wet conditions. PVA-DOPG hydrogels also significantly promoted lipophilic molecules’ penetration into stratum corneum (integrated fluorescence density of 6.95 ± 0.52 × 106 and mean fluorescence depth of 0.96 ± 0.07 mm) of ex-vivo porcine buccal mucosa (p < 0.001). Furthermore, PVA-DOPG hydrogels incorporating rapamycin inhibited malignant transformation of OLK mouse model induced by 4-Nitroquinoline N-oxide (4-NQO), distinct improvements in survival (the neoplasm incidence density at the 40th day is 0.0091) (p < 0.05), decrease in neoplasm incidence density of 36.36 % and inhibition rate in neoplasm volume of 75.04 ± 33.67 % have been demonstrated, suggesting the hydrogels were valuable candidates for potential applications in the management of OLK.

Engineered 1,6-heptadiynes based polymeric prodrug system for anticancer drug delivery

Diacetylene moiety, DIOL was functionalized to chemotherapeutic drug, chlorambucil and water-soluble moiety poly(ethylene glycol) to get our macromonomer MPDC. MPDC was further cyclopolymerized using Hoveyda Grubbs’ second generation catalyst, results to form polymer PMPDC. Amphiphilic nature of PMPDC leads to self-assembly in water which was characterized by dynamic light scattering and transmission electron microscope. Cytotoxicity study was performed with HeLa and MCF 7 cancer cell lines which showed good cell growth inhibition. As PMPDC having non-fluorescent property, another polymer PMPDP was synthesized as control using 1-pyrenebutyric acid which was further used for drug release at different pH and cell internalization study. Increase in internalization of polymer with increase in concentration was observed in both HeLa and MCF 7 cells. Formation of all the compounds were characterized carefully by different analytical techniques.

Construction and Evaluation of pH‐Responsive Nitrogen‐Containing Metal–Organic Frameworks as Oral Drug Carriers

ABSTRACTMetal–organic framework (MOF) is a porous material composed of metal ions/clusters and organic ligands. It has attracted much attention due to its high specific surface area, good biocompatibility, chemical modifiability, and diversity of components. Among many MOFs, zirconium‐based MOFs are particularly suitable for biological applications due to their optimal stability and low toxicity to hydrolysis. However, due to the weak coordination bonds between many metal clusters and organic ligands, most MOFs are prone to collapse in acidic environments, and the stability of MOFs as drug carriers cannot be guaranteed so that they cannot be widely used as oral drug carriers. This study synthesized the three MOFs using metal Zr ion clusters as the center and different nitrogen‐containing organic ligands, which are stable in gastric acid, namely, UiO‐66‐PDC, UiO‐66‐NH2, and UiO‐66‐NO2. The anionic drug loxoprofen (LOX) was loaded and characterized using scanning electron microscopy, infrared spectroscopy, thermogravimetric analysis, differential scanning calorimetry, and x‐ray diffraction. The adsorption and release behaviors of LOX and the three MOFs were studied from the molecular point of view by computer simulation. A series of behaviors and mechanisms of pH‐responsive nitrogen‐containing MOFs as oral drug carriers were further explored through rat pharmacokinetic experiments, the everted gut sac experiments, and intestinal absorption mechanism experiments. The experimental results show that there is a strong electrostatic interaction between anionic drug LOX and UiO‐66‐PDC under simulated gastric acid environment, which prolongs the half‐life of the drug, proving that LOX@UiO‐66‐PDC is a promising new oral drug delivery system.

Process Control of Multistep Surface Functionalization on Hydroxyethyl Starch Nanocapsules Determines the Reproducibility of the Biological Efficacy.

Nanocarrier synthesis is highly process-dependent, leading to potential batch-to-batch variability if it is not controlled at each step. This variability affects the reproducibility of subsequent biomodification, resulting in unpredictable biological effects, particularly for bioactive molecules such as interleukin-2 (IL-2). Inconsistent conjugation can lead to variable treatment outcomes and severe side effects. Therefore, precise control of each synthesis step is critical for ensuring a consistent quality and biological performance. Our study demonstrates that dividing nanocarrier synthesis into smaller, controlled steps improves reproducibility. Using this method, we achieved highly reproducible, concentration-dependent growth of CTLL-2 cells with hydroxyethyl starch (HES) nanocapsules functionalized with defined amounts of IL-2. We believe that such detailed, stepwise control in nanocarrier synthesis enhances batch consistency, improving the clinical applicability of the drug delivery systems.

Human epidermal growth factor receptor 2(Her2)-targeted pH-responsive MR/NIRF bimodal imaging-mediated nano-delivery system for the diagnosis and treatment of undifferentiated thyroid cancer.

Undifferentiated thyroid cancer (ATC) is highly malignant and does not respond well to sorafenib (SRF) treatment owing to the lack of specificity of SRF targeting. Drug delivery nanosystems can improve the efficiencies of drug in treating various cancer types. However, many conventional drug delivery nanosystems lack targeting and exhibit unresponsive drug release. Therefore, we developed a pH-responsive nano-targeted drug delivery systems using human serum albumin (HSA) as a carrier to generate manganese dioxide (MnO2)@HSA nanoparticles (NPs), then encapsulated SRF and the fluorescent dye indocyanine green (ICG) and finally modifyed the targeting antibody pertuzumab in the outer layer of the nano complexes, resulting in SRF/ICG/MnO2@HSA-pertuzumab (HISMP) NPs. This system targets human epidermal growth factor receptor 2 on the cell membrane surface of thyroid cancer cells and is designed to accumulate at tumor sites. Then, pH-responsive release of divalent manganese ions, ICG, and SRF enables magnetic resonance/fluorescence (MR/NIRF) dual-modality imaging and precise drug delivery for diagnostic and therapeutic integration. Various characterization analyses including transmission electron microscopy, Fourier infrared spectroscopy, and particle size analysis confirm that we successfully synthesized HISMP NPs with a diameter of 150.709nm. The results of CCK8 cytotoxicity and apoptosis assays show that HISMP NPs exhibited high cytotoxicity and induce apoptosis in thyroid cancer cells. In vivo MR/NIRF imaging experiments confirmed that the HISMP NPs specifically aggregated at tumor sites and have good in vivo MR/NIRF imaging ability and effective anti-tumor activity. The nano-delivery system is expected to provide a theoretical foundation for the efficient ATC diagnosis and therapy.

Recent Updates in Nanocrystal Technology: A Reference to Oral Drug Delivery System

Increasing the oral bioavailability of drugs that dissolve slowly may be possible with the use of nanocrystal technology. It is being employed for drug engineering and research after making rapid advancements in recent years. The manufacturing process for pharmaceuticals is significantly hampered by the low solubility and quick rate of dissolution of poorly soluble medications. When taken orally, medications that are poorly soluble often have low and inconsistent bioavailability, which could lead to therapeutic failure. Pure drug nanocrystals prepared via "bottom-up" or "topdown" procedu are able to significantly improve the way poorly soluble medications dissolve thanks to their enormous surface area, which in turn enhances oral absorption. Nanocrystal medications allow for the creation of various dosage formulations. The use of nanocrystal technology in pharmaceutical research, particularly for oral drug delivery systems, is the main focus of this review. First, a quick discussion on the characteristics of pharmaceutical nanocrystals and several nanocrystal technology preparation techniques is provided. The application of nanocrystal technology in pharmaceutical science is covered after a discussion of the creation of prolonged-release formulations. Next follows a brief overview of the scaling-up procedure, commercial nanocrystal drug products, and regulatory aspects of nanodrugs. This paper offers a thorough explanation of preparation techniques, their characterisation, and how they are used in oral drug delivery systems.

Development of a Bentonite Nanoparticle-Based Transdermal Drug Delivery System for Burn Wound Infection Prevention

Development of a Bentonite Nanoparticle-Based Transdermal Drug Delivery System for Burn Wound Infection Prevention

Development of FK506-loaded maleimide-functionalized cationic niosomes for prolonged retention and therapeutic efficacy in dry eye disease.

Tacrolimus (FK506) is widely used in ocular diseases such as corneal transplantation-host disease, uveitis, conjunctivitis, and dry eye disease (DED). However, its low aqueous solubility and poor ocular retention pose challenges for its application in the eye diseases. This study developed a novel FK506-loaded maleimide-functionalized cationic niosomes (FK506 M-CNS), aiming to prolong the retention time of FK506 in the eye and enhance its therapeutic efficacy. FK506 M-CNS had a particle size of 87.69 ± 1.05nm and zeta potential of 22.06 ± 1.01 mV. Results of histological evaluation through H&E staining and in vitro cytotoxicity of human corneal epithelial cells consistently revealed the excellent biocompatibility of FK506 M-CNS. FK506 M-CNS exhibited superior ocular retention compared to the market product Talymus®. FK506 M-CNS significantly alleviated the symptoms of DED and promoted the recovery of corneal epithelia. FK506 M-CNS group had the lowest expression levels of inflammatory factors associated with DED. These superiorities might be due to the electrostatic interaction between cationic niosomes and negatively charged mucin in the eye, and the covalent binding of maleimide with the thiol group in the mucin. The maleimide group improved the ocular retention and efficacy of FK506, but did not increase the toxicity. Results indicated that FK506 M-CNS had great potential as a nanopharmaceutical in the treatment of ocular diseases, and M-CNS could be a promising drug carrier for ophthalmic drug delivery systems.