Transdermal metformin

The transdermal drug delivery based on microneedles (MNs) provides a suitable and painless self-administration for diabetic patients. In this work, the hydrogel-forming MNs were firstly fabricated using PVA and chitosan (CS) as matrix. A hypoglycemic drug, metformin (Met), had been loaded into MIL-100(Fe). Then, both of free Met and Met-loaded MIL-100(Fe) were integrated into hydrogel-forming MNs for regulation of BGLs on diabetic rats. After penetrated into the skin, the free Met could be firstly released from MNs...

Diabetes currently affects approximately 500 million people worldwide and is one of the most common causes of mortality in the United States. To diagnose and monitor diabetes, finger-prick blood glucose testing has long been used as the clinical gold standard. For diabetes treatment, insulin is typically delivered subcutaneously through cannula-based syringes, pens, or pumps in almost all type 1 diabetic (T1D) patients and some type 2 diabetic (T2D) patients. These painful, invasive approaches can cause non-adherence to glucose testing and insulin therapy...

Obesity is a severe public health problem. Healthy lifestyle interventions are commonly recommended for fighting obesity. But they are hard to follow and have low efficacy. Pharmacotherapy and surgery are of high efficacy but are beset with side effects. Browning subcutaneous white adipose tissue (WAT) is a practical and efficient approach for combating obesity. Metformin, a commonly used FDA-approved antidiabetic drug, is potent to induce browning of WAT through phosphorylation and activation of AMP-activated protein kinase...

Diabetes mellitus is an irreversible, chronic metabolic disorder indicated by hyperglycemia. It is now considered a worldwide pandemic. T2DM, a spectrum of diseases initially caused by tissue insulin resistance and slowly developing to a state characterized by absolute loss of secretory action of the β cells of the pancreas, is thought to be caused by reduced insulin secretion, resistance to tissue activities of insulin, or a combination of both. Insulin secretagogues, biguanides, insulin sensitizers, alpha-glucosidase inhibitors, incretin mimetics, amylin antagonists, and sodium-glucose co-transporter-2 (SGLT2) inhibitors are the main medications used to treat T2DM...

The most common reason for metformin incompliance is due to its side-effect profile. Metformin can cause issues with the gastrointestinal tract and result in nausea, abdominal pain, diarrhea, bloating, or vomiting. The size of the metformin tablet, which is quite large, is another reason for incompliance. Compounding pharmacists can prepare a topical formulation of metformin, which helps eliminate the unwanted gastrointestinal side effects, as well as eliminate the incompliance due to the size of the tablet...

Psoriasis and diabetes are both common comorbidities for each other, where inflammation and insulin resistance act in a vicious cycle, driving the progression of disease through the activation of the NF-κB signaling pathway. Therefore, disrupting the linkage between inflammation and insulin resistance by inhibiting the NF-κB pathway presents a promising therapeutic strategy for addressing psoriasis-diabetic comorbidity. Herein, an open-loop therapy was developed by integrating microneedle-mediated short- and long-range missiles to target psoriasis and diabetes, respectively...

Herein we designed, optimized, and characterized the Metformin Hydrochloride Transethosomes (MTF-TES) and incorporate them into Chitosan gel to develop Metformin Hydrochloride loaded Transethosomal gel (MTF-TES gel) that provides a sustained release, improved transdermal flux and improved antidiabetic response of MTF. Design Expert® software (Ver. 12, Stat-Ease, USA) was applied for the statistical optimization of MTF-TES. The formulation with Mean Particle Size Distribution (MPSD) of 165.4 ± 2...

The release of metformin, a drug used in the treatment of cancer and diabetes, from poly(2-hydroxyethyl methacrylate), pHEMA, hydrogel-based microneedle patches is demonstrated in vitro. Tuning the composition of the pHEMA hydrogels enables preparation of robust microneedle patches with mechanical properties such that they would penetrate skin (insertion force of a single microneedle to be ≈40 N). Swelling experiments conducted at 20, 35, and 60 °C show temperature-dependent degrees of swelling and diffusion kinetics...

Type 2 diabetes is one of the major challenges that the world is facing today. However, metformin (MET) as most type 2 diabetics' first-line oral hypoglycemic drug may cause serious side effects such as gastrointestinal irritation and nausea which reduce the patients' medication compliance. Therefore, the aim of the study was to design a safe and effective self-treatment device for the delivery of MET. Here, a kind of coated microneedle (MN) patches based on poly(ethylene glycol)diacrylate (PEGDA) were prepared by a two-step casting method and photopolymerization process for transdermal administration of MET...

Diabetes chronic wound is a severe and frequently occurring medical issue in patients with diabetes that often leads to more serious complications. Microneedles (MNs) can be used for wound healing as they can effectively pierce the epidermis and inject drugs into the wound tissue. However, common MN patches cannot provide sufficient skin adhesion to prevent detachment from the wound area. Inspired by the barb hangnail microstructure of porcupine quills, a porcupine quill-like multilayer MN patch with an adhesive back patching for tissue adhesion and diabetic wound healing was designed...

Diabetes mellitus (DM) is a metabolic disorder that is one of the most common health problems in the world, primarily type 2 DM (T2DM). Metformin (MTF), as the first-line treatment of DMT2, is effective in lowering glucose levels, but its oral administration causes problems, including gastrointestinal side effects, low bioavailability, and the risk of hypoglycemia. In this study, we formulated MTF into microparticles incorporating a glucose-responsive polymer (MP-MTF-GR), which could potentially increase the bioavailability and extend and control the release of MTF according to glucose levels...

This study evaluated the potential of monoolein (MO)-based nanodispersions to promote the cutaneous co-delivery of metformin (MET) and methylene blue (MB) for the treatment of non-melanoma skin cancer. MO-based nanodispersions were obtained using Kolliphor P407 (KP) and/or sodium cholate (CH), and characterized concerning the structure, thermal stability, ability to disrupt the skin barrier, cutaneous permeation and retention of MB and MET. Additionally, the cytotoxic effect of MO nanodispersions-mediated combination therapy using MET and MB in A431 cells was evaluated...

Transdermal drug delivery system (TDDS) is the system for transmitting a drug through the skin into the blood circulation. In this work, κ-Carrageenan (κC) was used as the drug matrix material. The porous κC matrices were fabricated by dissolving the κC in deionized water to obtain hydrogels and then using the freeze-dryer to obtain cryogels. The porous (κC) matrices showed interconnected pore sizes varying between 6.05 to 25.8 nm. In the drug release experiments, the drug diffusion coefficient increased and the drug release duration was reduced with decreasing κC concentration due to the larger κC pore sizes...

PURPOSE: The purpose of the present study was to explore the feasibility of transdermal delivery of metformin, a commonly used oral antidiabetic drug, by ionic liquid (IL) technology. METHODS: Metformin hydrochloride (MetHCl) was first transformed into three kinds of ILs with different counterions. The physicochemical properties of the obtained ILs were characterized in depth. The simulation of stable configuration and calculation of interaction energies were conducted based on density functional theory (DFT)...

Obesity is a serious public health problem that is strongly associated with increased multiple comorbidities such as diabetes, cardiovascular disease, and some types of cancer. While current anti-obesity treatments have various issues, locally transforming energy-storing white adipose tissue (WAT) into energy-burning brown-like/beige adipose tissue, the so-called browning of WAT, has been suggested to enhance obesity treatment efficiency with minimized side effects. Metformin is a first-line antidiabetes drug and a potent activator of AMP-activated protein kinase...

INTRODUCTION: Metformin hydrochloride (metformin HCL), a first-line drug treating diabetes type II, was known to cause severe gastritis, so seeking a non-oral dosage form was the new trend. Bilosomes are bilayer nano-vesicles of non-ionic surfactants embodying bile salts. In our study, bilosomes were investigated as an acceptable novel carrier for active targeting transdermal delivery of metformin HCL, circumventing its side effects. METHODS: Twelve bilosome formulations were prepared with solvent evaporation method with slight modification according to a 31 ...

5-aminolevulinic acid (ALA)-mediated photodynamic therapy (PDT) has emerged as a promising therapy for hypertrophic scar (HS). However, the poor permeability of ALA across biological barriers and pro-survival autophagy of fibroblasts largely restricted the efficacy of PDT. Herein, PDT was well equipped with spear and shear to overcome the therapeutic resistance. Specifically, hyaluronidase (HAase) based dissolving microneedles (MN)with improved stiffness and permeability were developed as a spear to deliver ALA into deep lesions by combating the dual barriers of stratum corneum and dense extracellular matrix (ECM)...

In this work, the rapidly separable microneedles (MNs) consisted of needle-tips and supporting bases have been fabricated by a step-by-step coating method. Poly (vinyl alcohol) (PVA) have been used to prepare the needle-tips of MNs in which they are capped on the solvable supporting bases consisted of sodium bicarbonate, poly (vinyl pyrolidone) (PVP), and tartaric acid (TA) (NaHCO3 /PVP/TA). After insertion into the skin, the needle-tips can be separated rapidly from the patches within 90 s due to the generation of air bubbles in the supporting bases by the reaction between NaHCO3 and TA after absorption of tissue fluid, leading to the needle-tips remaining in the skin tissue...

To enhance the compliance of drug delivery for patients, the novel near-infrared (NIR) light-triggered and separable microneedles (MNs) have been developed in this work. Firstly, prussian blue nanoparticles (PB NPs) as the photo-thermal conversion factor and metformin as the hypoglycemic drug were embedded into the separable arrowheads, which consisted by poly (vinyl alcohol) and sucrose (PVA/Suc). The arrowheads of MNs were located on soluble solids supporting substrates that produced by poly(vinyl pyrrolidone) (PVP)...

Drug loaded hydrogels have proven to be versatile controlled-release systems. We report here on heat active hydrogel formation by mixing graphene oxide (GO) or carboxyl enriched reduced graphene oxide (rGO-COOH) with metformin hydrochloride, an insulin sensitizer drug currently used as the first line therapy to treat patients with type 2 diabetes. The driving forces of the gelation process between the graphene-based nanomaterial and metformin are hydrogen bonding and electrostatic interactions, weakened at elevated temperature...