Drug delivery and therapeutic challenges of gliclazide, a BCS class II drug used in type 2 diabetes mellitus (T2DM) can be overcome by exploring smarter carriers of second-generation nanocrystals (SGNCs). A combined method of emulsion diffusion, high-pressure homogenization and solvent evaporation method were employed in the preparation of gliclazide loaded poly (D, L-lactide-co-glycolide) (PLGA) SGNCs. Taguchi experimental design was adopted in fabrication of Gliclazide SGNc using Gliclazide -PLGA ratio at 1:0.5, 1:0.75, 1:1 with stabilizer (Poloxamer-188, PEG 4000, HPMC E15 at 0.5, 0.75, 1% w/v). The formulated gliclazide of SGNCs were investigated for physicochemical properties, in vitro drug release, and in vivo performance studies using type-2 diabetes rat model. The formulation (SGNCF1) with Drug: PLGA 1: 0.5 ratio with 0.5% w/v Poloxamer-188 produced optimized gliclazide SGNCs. SGNCF1 showed spherical shape, small particle size (106.3 ± 2.69 nm), good zeta potential (−18.2 ± 1.30 mV), small PDI (0.222 ± 0.104) and high entrapment efficiency (86.27 ± 0.222%). The solubility, dissolution rate and bioavailability of gliclazide SGNCs were significantly improved compared to pure gliclazide. The findings emphasize gliclazide SGNCs produce faster release initially, followed by delayed release with improved bioavailability, facilitate efficient delivery of gliclazide in T2DM with better therapeutic effect.
29 October 2018 in Nano Biomedicine and Engineering
Over the past few decades, there has been an increased interest for innovative drug delivery systems to improve safety, efficacy and patient compliance, thereby increasing the product patent life cycle. The discovery and development of new chemical entities is not only an expensive but also time consuming affair. Hence the pharmaceutical industries are focusing on the design and development of innovative drug delivery systems for existing drugs. One such delivery system is the fast disintegrating oral film, which has gained popularity among pediatric and geriatric patients. This fast disintegrating film with many potential benefits of a fast disintegrating tablet but devoid of friability and risk of choking is more acceptable to pediatric and geriatric patients. Formulation of fast disintegrating film can be achieved by various techniques, but common methods of preparation include spraying and casting. These film forming techniques use hydrophilic film former in combination with suitable excipients, which allow the film to disintegrate or dissolve quickly in the mouth within a few seconds without the administration of water. In view of the advantages of the fast disintegrating films over the fast disintegrating tablets and other dosage forms, it has the potential for commercial exploitation. The oral film dosage form not only has certain advantages of other fast disintegrating systems but also satisfies the unmet needs of the market. The present review emphasizes on the potential benefits, design and development of robust, stable, and innovative orally fast- disintegrating films and their future scenarios on a global market as a pharmaceutical dosage form.
A fast, sensitive, and specific reversed-phase high-performance liquid chromatographic (RP-HPLC) method for the determination of letrozole in Wistar rat serum was developed. In this method, liquid-liquid extraction of letrozole was achieved using diethyl ether as the extracting solvent. The analysis was carried out on a reversed-phase C18 (250 mm × 4.6 mm, 5 μm) column with an isocratic mobile phase of methanol-water (70:30,v/v), at a flow rate of 1.0 mL min(-1). Detection was carried out at 239 nm with a UV-visible spectrophoto-metric detector. The method was shown to be selective and linear over the concentration range of 0.15-100 μg mL(-1). The intra-day and inter-day precision studies showed good reproducibility with coefficients of variation less than 11% for the analyte. The relative errors of intra- and inter-day accuracy were within -11.52 to -2.26%. The limit of quantification was evaluated to be 0.15 μg mL(-1). The method was successfully applied for the pharmacokinetic study of letrozole after oral administration of 10 mg kg(-1) of letrozole in six healthy Wistar rats.
5 March 2022 in International Journal of Environmental Health Research
The coronavirus disease 2019 (COVID-19) has caused a worldwide outbreak. The severe acute respiratory syndrome coronavirus 2 virus can be transmitted human-to-human through droplets and close contact where personal protective equipment (PPE) is imperative to protect the individuals. The advancement of nanotechnology with significant nanosized properties can confer a higher form of protection. Incorporation of nanotechnology into facemasks can exhibit antiviral properties. Nanocoating on surfaces can achieve self-disinfecting purposes and be applied in highly populated places. Moreover, nano-based hand sanitizers can confer better sterilizing efficacies with low skin irritation as compared to alcohol-based hand sanitizers. The present review discusses the incorporation of nanotechnology into nano-based materials and coatings in facemasks, self-surface disinfectants and hand sanitizers, in the hope to contribute to the current understanding of PPE to combat COVID-19.
Poor solubility, erratic bioavailability and delivery challenges associated with gliclazide, which is commonly used in type 2 diabetes mellitus (T2DM) treatment, are overcome by exploring electrospun nanofibers technology. Employing emulsion electrospinning method with polyvinyl alcohol (PVA) alone and in combination with poly(d/l-lactide-co-glycolide) (PLGA), nanofibers were fabricated. Different concentrations of PLGA at 0.05%, 0.10% and 0.15% w/v were added to PVA to achieve a modified drug release profile to meet the typical physiological needs of T2DM, such as a faster drug release at meals followed by prolonged release to maintain constant plasma glucose level, which is highly desirable in T2DM management. Fabricated gliclazide-nanofibers were characterized by various studies, such as solubility, in-vitro drug release, drug release kinetic, scanning electron microscopy (SEM), differential scanning calorimetric (DSC), and Fourier transform infrared (FTIR) spectroscopy. GLZNF2, formulation of Drug:PVA:PLGA 0.1:10:0.05% w/v produced optimized gliclazide nanofibers. The optimized GLZNF2 nanofibers were incorporated into gelatin capsule for oral administration. SEM image of optimized formulation (GLZNF2) shows cylindrical shaped fiber, indicating gliclazide incorporated homogeneously in polymers with average fiber diameter 4.357 ± 0.83 µm. The solubility and dissolution rate of gliclazide nanofibers significantly improved compared to pure gliclazide. The gliclazide nanofibers produce a biphasic drug release profile, initial fast release, followed by prolonged release. Oral fabricated gliclazide fibers have tremendous potential as a drug carrier, and alternative technology for the improvement of solubility, dissolution rate, reduction in the dosing frequency and better blood glucose control could be explored in T2DM management.