Current drug delivery最新文献

Introduction: The incidence and mortality rates of liver cancer are high; therefore, developing new drug delivery systems with good biocompatibility and targeting has become a research hotspot.

Methods: Mitoxantrone hydrochloride (MH) loaded in acidic Panax notoginseng polysaccharide III nanoparticles (MANPs) was prepared using electrostatic adsorption. This was achieved by loading MH in acidic Panax notoginseng polysaccharide III (APPN III), a natural compound that exhibits anti-tumor activity. Response surface methodology was used to determine the parameters for the best formulation.

Results: Fourier-transform infrared spectroscopy and differential scanning calorimetry indicated that MH in MANPs was amorphous and exhibited good encapsulation efficiency in the carrier. Findings from dynamic dialysis confirmed that MANPs exhibited slow drug release at pH 6.8 and over the pH range of 7.2-7.4. In vitro experiments confirmed the anti-tumor effects of MANPs on H22 cells based on the inhibition of cell proliferation and an increase in apoptosis. MANPs also demonstrated an obvious anti-tumor effect without any toxicity in H22 tumor-bearing mice. This effect could be attributed to APPN III enhancing the immune system and exerting a synergistic anti-tumor effect in combination with MH, thereby alleviating MH-induced damage to the immune system in H22 tumorbearing mice.

Conclusion: As a nano-carrier prepared using natural resources, APPN III shows immense potential in the field of drug delivery and could serve as a novel option for the effective delivery of chemotherapeutic drugs.

Malaria is still a major endemic disease transmitted in humans via Plasmodium-infected mosquitoes. The eradication of malarial parasites and the control measures have been rigorously and extensively deployed by local and international health organizations. Malaria's recurrence is a result of the failure to entirely eradicate it. The drawbacks related to malarial chemotherapy, non-specific targeting, multiple drug resistance, requirement of high doses, intolerable toxicity, indefinable complexity of Plasmodium's life cycle, and advent of drug-resistant strains of P. falciparum are the causes of the ineffective eradication measures. With the emergence of nanotechnology and its application in various industrial domains, the rising interest in the medical field, especially in epidemiology, has skyrocketed. The applications of nanosized carriers have sparked special attention, aiming towards minimizing the overall side effects caused due to drug therapy and avoiding bioavailability. The applications of concepts of nanobiotechnology to both vector control and patient therapy can also be one of the approaches. The current study focuses on the use of hybrid drugs as next-generation antimalarial drugs because they involve fewer drug adverse effects. The paper encompasses the numerous nanosized delivery-based systems that have been found to be effective among higher animal models, especially in treating malarial prophylaxis. This paper delivers a detailed review of diagnostic techniques, various nanotechnology approaches, the application of nanocarriers, and the underlying mechanisms for the management of malaria, thereby providing insights and the direction in which the current trends are imparted from the innovative and technological perspective.

Introduction: Psoriasis is a chronic inflammatory skin disorder that poses significant challenges regarding effective and targeted drug delivery. Bioactive substances like betulin have shown tremendous utility in treating these conditions; however, they pose limited utility owing to their physicochemical characteristics. Here, we aimed to develop a novel topical dosage form for treating psoriasis, utilising betulin-loaded Nanostructured lipid carriers (NLCs) incorporated into a hydrogel matrix.

Methods: The optimization of the formulation was meticulously conducted using a design expert-13 software, and its diverse physicochemical attributes were thoroughly examined. Evaluating betulin's in vitro release pattern from the NLC-hydrogel demonstrated consistent and regulated drug release properties. Additionally, the formulation demonstrated improved skin penetration abilities as determined by in vitro skin permeation experiments employing Franz diffusion cells-furthermore, the therapeutic effectiveness of the betulin-NLC-hydrogel was assessed by an in vivo experiment carried out using an imiquimod-induced psoriasis-like skin inflammation model in BALB/c female mice.

Results: The NLCs exhibited a pH of 5.67±0.86, particle size of 148.16±12.66 nm, and zeta potential of -22.84±2.37 mV, ensuring stability and suitability for topical use. The gel, with a pH of 6.05±0.43 and viscosity of 17550±120 cPs, showed enhanced skin hydration and lipid restoration. Drug release studies indicated a slower release from NLCs and gel, improving skin retention. Stability tests revealed that the formulations were stable at room temperature but not at elevated temperatures. The in vitro safety profile of the formulation revealed no significant adverse effects on HaCaT cell lines. The NLC gel demonstrated significant anti-psoriatic activity, reducing inflammation and cytokine levels.

Conclusion: The betulin-NLC-hydrogel formulation exhibited promising characteristics for the topical treatment of psoriasis, showcasing optimised drug delivery, sustained release, and notable therapeutic efficacy. The findings from this study provide a foundation for the potential clinical translation of this innovative topical dosage form for improved psoriasis management.

Background: Fungal keratitis (mycotic keratitis) is an eye infection in which the cornea is infected by fungi and such fungal keratitis management can be effectively possible by ocular administration of antifungal drugs.

Objective: The main objectives of the present research were to develop and evaluate fluconazoleloaded transfersomal hydrogels for ocular delivery in the effective management of fungal keratitis.

Methods: A 2³ factorial design-based approach was used for statistical optimization, where (A) the ratio of lipid to edge activators, (B) the amount of hyaluronic acid (% HA), and (C) the ratio of edge activators (sodium deoxycholate to Span 80) were taken as three factors. The average vesicle diameter (Z, nm) of transfersomes was taken as a response. Further, fluconazole-loaded transfersomes (FTO) were incorporated into 1% Carbopol 940-based hydrogel (OF1) and 2% HMPC K4M-based hydrogel (OF2) containing D-panthenol (5% w/w).

Results: The optimal variable setting for the optimized formulations of FTO was (A) = 9.15, (B) = 0.30%, and (C) = 3.00. FTO exhibited 66.39 nm Z, 0.247 polydispersity index, - 33.10 mV zeta potential, and 65.38 ± 1.77 % DEE, and desirable elasticity. TEM image of FTO demonstrated a unilamellar vesicular structure. The ex vivo ocular permeation of fluconazole from transfersomal hydrogels was sustained over 24 h. All the transfersomal hydrogels showed good bioadhesion and excellent antifungal activity with respect to the zone of inhibition against Candida albicans than Aspergillus fumigates, in vitro. HET-CAM study results demonstrated that both the hydrogels were nonirritant and safe for ocular. Short-term physical stability study suggested the stability of the developed formulation.

Conclusion: The current research demonstrated a new way to enhance the ocular penetration of fluconazole via transfersomal hydrogel formulations for ocular delivery in the effective management of fungal keratitis.

Nanostructured lipid carriers (NLCs) are lipidic nanocarriers that recover the permanency and capacity of drug payloads. NLCs are well-known as second-generation lipid nanocarriers with an unstructured matrix, presenting potentially advantageous nanocarrier systems with marketable opportunities because of reproducible production methodologies and biocompatible lipidic excipients. These (NLCs) are now recognized as a very promising nanocarrier structure for the efficient delivery of drugs via different administration routes. In recent years, several NLC-based gels have been developed and evaluated for topical delivery of many drugs and other therapeutic agents. This review article presents an overview of NLC-based topical gels investigated to deliver drugs via ocular, dermal, and transdermal routes. In addition, the classification, manufacturing, characterizations, advantages, and disadvantages of NLCs are addressed in this article. We also discussed different evaluations of NLC-based topical gels.

Insulin is a peptide hormone that is essential for regulating body homeostasis. Furthermore, it is involved in various neurological functions such as memory, behaviors, and cognition. The ubiquitous distribution of insulin receptors on various brain cells, such as neurons, microglia, astrocytes, and oligodendrocytes, and their differential localization across various brain regions, including the hippocampus, hypothalamus, and olfactory bulb, collectively underscore the crucial involvement of insulin in the modulation of cerebral functions. Along with ageing, in some pathological conditions such as diabetes and brain insulin resistance, the need for exogenous insulin is felt to compensate for insulin deficiency. In these cases, the biggest obstacle to the delivery of insulin to the brain is the blood-brain barrier (a physical barrier consisting of endothelial cells with tight junctions), which prevents the direct entry of most substances possessing high molecular weight, like insulin, into the brain. Therefore, different delivery methods have been proposed by researchers for insulin delivery that directly or indirectly cause the transfer of insulin to the brain. Some of these methods lack high efficiency and cause many side effects for the patient. In this regard, many new technologies have come to the aid of researchers and have introduced more effective delivery strategies, including the use of nanocarriers. Despite the promising outcomes demonstrated in the experimental models, the utilization of these techniques in human studies remains at a nascent stage and necessitates further comprehensive investigation. This review article aims to examine the diverse methods of insulin administration to the brain by gathering extensive information on insulin and its obstacles to brain delivery.

Drug transporters are critical factors influencing the pharmacokinetics of drugs under hypoxic conditions. Studies have shown significant changes in drug transporter levels in the hypoxic environment. In addition to being regulated by HIF-1, nuclear receptors, and inflammatory factors, hypoxia can also regulate transporters through epigenetic modifications, thereby affecting drug absorption, distribution, metabolism, and excretion. In recent years, increasing attention has been paid to the role of epigenetic modifications in regulating drug transporters under hypoxic conditions at high altitudes. In this study, we comprehensively review the effects of hypoxia on drug transporters and epigenetic modifications and explore the regulatory mechanism of epigenetic modifications on drug transporter expression under hypoxic conditions. The aim is to provide a reference for exploring the epigenetic regulation mechanism of drug transporter expression in the hypoxic environment at high altitudes, guide the study of pharmacokinetics, and promote effective and safe medication at high altitudes.

Introduction: Nanofiber (NF) films have emerged as a promising alternative for treating psoriasis. Based on their specific characteristics, they have distinguished themselves from other topical dosage forms, such as hydrogels, foams, and sponges. This research looks at making biocompatible and biodegradable nanofibers out of polyvinyl alcohol (PVA) and gelatin and adding hesperidin (HPN) and ofloxacin (OFX) as medicine.

Methods: HPN-OFX-integrated nanofiber (HPN-OFXNF) films were prepared using electrospinning. Subsequently, the surface morphology, entrapment efficiency, in vitro drug diffusion, and antimicrobial, anti-inflammatory, and anti-psoriasis properties were investigated.

Results: Scanning electron microscopy (SEM) analysis revealed that the produced nanofibers exhibited smooth surfaces with diameters from 50.67 to 114.4 nm, entrapment efficiencies from 69.3 ± 1.8% for OFX and 45.63 ± 1.6% for HPN. At the end of 48 h, nanofibers showed 90.8 ± 2.4% of OFX and 97.3± 3.1% of HPN release. In vitro, antimicrobial testing of the films demonstrated 24.89 ± 3.2 and 42.46 ± 4.4 mm zones of inhibition against E. coli and S. aureus. The total antioxidant activity of HPN is 198.67±2.38 (μ mol AAE/mg HPN), and HPN-OFXNF is 271.12 ± 3.56 (μ mol AAE/mg HPN-OFXNF), and their IC50 values against HaCaT cell growth of 80.5 ± 2.5 and 64.6 ± 3.4 μg/ml, respectively.

Discussion: HPN-OFXNFs have been developed successfully by the electrospinning method with moderate entrapment efficiencies, showing a biphasic trend of an early burst trailed by a sustained pattern of drug release, depending on the surface area and diameter of the fibers. Enhanced zones of inhibition and anti-inflammatory efficacy of NFs in comparison with their pure counterparts have been demonstrated to be beneficial. Stronger antioxidant efficacy, inducing anti-proliferation and promoting apoptosis in human keratinocytes, has made them the best versions over pure drug compounds.

Conclusion: This therapy, which includes a combined anti-inflammatory and antibacterial treatment strategy with an innovative drug delivery system, has proven to be a promising development in treating psoriasis.

The field of fiber technology is a dynamic and innovative domain that offers novel solutions for controlled and targeted therapeutic interventions. This abstract provides an overview of key aspects within this field, encompassing a range of techniques, applications, commercial developments, intellectual property, and regulatory considerations. The foundational introduction establishes the significance of fiber-based drug delivery systems. Electrospinning, a pivotal technique, has been explored in this paper, along with its various methods and applications. Monoaxial, coaxial, triaxial, and side-by-side electrospinning techniques each offer distinct advantages and applications. Centrifugal spinning, solution and melt blowing spinning, and pressurized gyration further contribute to the field's diversity. The review also delves into commercial advancements, highlighting marketed products that have successfully harnessed fiber technology. The role of intellectual property is acknowledged, with patents reflecting the innovative strides in fiber-based drug delivery. The regulatory perspective, essential for ensuring safety and efficacy, is discussed in the context of global regulatory agencies' evaluations. This review encapsulates the multidimensional nature of fiber technology in drug delivery and pharmaceuticals, showcasing its potential to revolutionize medical treatments and underscores the importance of continued collaboration between researchers, industry, and regulators for its advancement.