Therapeutic delivery最新文献

Orodispersible film (ODF) is one of the novel formulations that disintegrate rapidly in the mouth without the requisite for water compared to other conventional oral solid dosage formulations. This delivery system serves as a convenient mode of administration, especially in patients who have dysphagia and fluid restriction, being beneficial to pediatric, geriatric, and bedridden patients. A novel sildenafil ODF containing sildenafil citrate is formulated to be used in patients with erectile dysfunction (ED). This review discusses the advantages of ODF in improving compliance and satisfaction in these patients and describes the manufacturing techniques, evaluation tests, bioequivalence, and stability studies of sildenafil ODF. This formulation offers unique benefit to patients with ED by improving their acceptance and compliance and respecting their privacy and the need for a discreet treatment. Moreover, the comparison of pharmacokinetic parameters between the sildenafil ODF administered with and without water and the conventional film-coated tablet were similar. It also demonstrated reliable performance that yielded a consistent product, meeting all specifications at release and after three weeks of storage under stressed conditions (60°C). Sildenafil ODF warrants improved ease of intake, taste, portability, storage, and compliance among ED patients, making it the potential most preferred formulation and drug of choice.

Introduction: Lysozyme is a globular hydrolytic enzyme whose tissue level is imperative for various clinical diagnostics. High levels of lysozyme are related to several inflammatory disorders, that breakdown cartilaginous tissues. Recently nanostructures have become widely used as modulators for enzyme activity.

Areas covered: This study delves into the influential role played by surface-modified iron oxide nanoparticles (IONPs) as novel lysozyme nano-inhibitors. Stern-Volmer plots results for lysozyme interaction with Cit-IONPs and Thy-IONPs reveal dynamic quenching constant (KSV) of 40.075 and 65.714 ml/mg, binding constant (Kb) of 1.539 × 103 and 4.418 × 103 ml/mg, and binding free energy (∆G°binding) of -43.563 KJ. mol^-1 and -49.821 KJ. mol^-1, respectively. Upon interaction with IONPs, the catalytic activity of lysozyme decreases due to conjugation with Thy-IONPs and Cit-IONPs compared to the free form of the enzyme. Computational approaches show that the citrate and thymoquinone molecules have binding affinities with lysozyme active residues of about -4.3 and -4.7 kcal/mol, respectively.

Expert opinion/commentary: Both formulations of IONPs demonstrate high affinity toward lysozyme proteins. This work shows a higher binding affinity between lysozyme and Thy-IONPs than with Cit-IONPs. These findings suggest that Thy-IONPs represent a promising class of nano-inhibitors for lysozyme, opening new avenues for treating disorders associated with lysozyme overexpression.

Ovarian cancer remains one of the main causes of human mortality, accounting for millions of deaths every year. Despite of several clinical options such as chemotherapy, photodynamic therapy (PDT), hormonal treatment, radiation therapy, and surgery to manage this disease, the mortality rate is still very high. This alarming statistic highlights the urgent need for innovative approaches to improve both diagnosis and treatment. Success stories of iron oxide nanoparticles, i.e. Ferucarbotran (Resovist®) and Ferrixan (Cliavist®) for liver imaging, CNS (Central nervous system) imaging, cell labeling, etc. have motivated researchers to explore these nanocarriers for treatment and diagnosis of different diseases. Iron oxide nanoparticles have improved the therapeutic efficacy of anticancer drugs through targeted delivery, heat/ROS (reactive oxygen species) generation on application of external energy and have also shown great potential as contrast agents for magnetic resonance imaging (MRI). Their unique magnetic properties enable sensitive imaging, and surface modification allows the attachment of specific biomolecules for targeted detection of ovarian cancer cells. Their unique properties, viz. magnetic responsiveness and surface functionalization, make them versatile tools for enhancing both imaging and therapeutic outcomes. Present article reviews the literature on the synthesis, functionalization, and applications of iron oxide nanoparticles in management of ovarian cancer.

Many therapeutic applications use the transdermal method to avoid the severe restrictions associated with oral medication delivery. Given the limitations of traditional drug delivery via skin, transdermal microneedle (MN) arrays have been reported to be versatile and very efficient devices due to their outstanding characteristics such as painless penetration, affordability, excellent medicinal efficacy, and relative safety. MNs have recently received increased attention for their ability to cure vascular illnesses such as hypertension and thrombosis, as well as promote wound healing via the angiogenesis impact. The integrant of method manufacturing and biodegradable material allows for the modification of MN form and drug release pattern, hence increasing the flexibility of such drug delivery. In this review, we focused on recent improvements in MN-mediated transdermal administration of protein and peptide medicines for improved functional angiogenesis and vascular therapy. We also provide an overview of the present applications of MNs-mediated transdermal protein and peptide administration, particularly in the realm of vascular system disease therapy. Finally, the current state of clinical translation and a forecast for future progress are provided.

Aims: The present investigation aimed at the comparative evaluation of the developed nanocarriers, viz. spherulites and cubosomes for lung targeting.

Materials and methods: Both the spherulites and cubosomes were characterized for their entrapment efficiency, drug loading, size and zeta potential, in-vitro drug release profile, surface morphology, hemocompatibility, and in-vivo pharmacokinetic and lung biodistribution.

Results and conclusions: The optimized batches of spherulites and cubosomes possessed high entrapment efficiency and drug loading with size around 200 nm, which is suitable for lung targeting. The zeta potential value for both the nanoformulations was found to be between -20 and -30 mv indicating the physical stability against aggregation. The SEM and TEM analysis revealed the presence of spherical and discrete particles in both the types of nanocarriers. Water channels were observed in case of cubosomes. Spherulites and cubosomes showed pH-dependent drug release with lower release at physiological pH while higher release at the pH of the tumor microenvironment. Both spherulites and cubosomes exhibited highly significant increase in the half-life and mean residence time in the plasma. The prepared nanoformulations were hemocompatible and had higher lung targeting potential compared to the plain drug solution.

Background: This study aimed to develop and analyze nystatin:β-cyclodextrin and chlorhexidine:β-cyclodextrin mucoadhesive hydrogels.

Materials & methods: Hydrogels were characterized by in vitro and ex vivo analyses, and antifungal activity against Candida albicans.

Results: The hydrogel showed high adhesiveness and retention (83.37 ± 2.05%) to the porcine oral mucosa. The drug release from complexed nystatin and chlorhexidine hydrogels was 1.5 (95 µg/cm²) and 4.0 times higher (800 µg/cm²) than non-complexed drugs. Rheological studies indicated the prevalence of elastic behavior of the formulations. Ex vivo permeation using porcine mucosa showed retention on the oral mucosa. Hydrogels with nystatin and chlorhexidine inclusion complex showed inhibition percentages of 88.87% and 91.57%, respectively, and median inhibition zones of 8 mm.

Conclusion: Mucoadhesive hydrogels with inclusion complex are promising for oral lesions with greater retention at the treatment site.

Localized disorders, even though originally confined to a specific body part, can progress into potentially life-threatening systemic disorders if treated inappropriately. Local treatment is often highly challenging due to poor penetration of therapeutic agents from their vehicles into the affected body site. Systemic treatment on the other hand often comes with unspecific side effects. The skin is the largest organ of the body, and conditions such as wounds and bacterial or fungal infections disrupt its natural barrier properties, important for the homeostasis of the human body. Advanced drug delivery systems for treating these conditions could greatly improve the treatment outcome and patient compliance. Other parts of the body that are of interest regarding localized treatment are, for example, the eyes along with mucosal tissues which are present in the vagina and lungs. Rather than focusing on specific diseases or parts of the body, this review provides an overview of the different drug delivery platforms that have been employed for enhanced local treatment. The following systems will be discussed: nanoparticle-based systems, such as nanocrystals, polymeric, lipidic, and inorganic nanoparticles, and nanogels; cyclodextrin inclusion complexes; and several devices like microarray patches, wound dressings, and films.