Preparation, Characterization, and In Vivo Pharmacokinetic Evaluation of Polyvinyl Alcohol and Polyvinyl Pyrrolidone Blended Hydrogels for Transdermal Delivery of Donepezil HCl

Bashyal, Santosh; Shin, Chang Yell; Hyun, Sang Min; Jang, Sun Woo; Lee, Sang Kil

doi:10.3390/pharmaceutics12030270

Cited by 24 publications

(9 citation statements)

References 48 publications

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“…Ex vivo buccal permeability studies were conducted as illustrated in Figure 1. Permeability assays of the elastic liposomes (SC-EL and SGDC-EL) were conducted across porcine buccal tissues using a vertical static Franz diffusion cell (GlaxoSmithKline, Harlow, UK; 0.79 cm 2 diffusion area), as described previously [30]. Studies were performed in the direction of the donor to receptor compartment, and the porcine buccal tissue was placed within the donor and receptor compartments of the Franz diffusion cell system, with constant magnetic stirring (600 rpm) at 37 • C. The insulin solution (500 µL), SC-EL, or SGDC-EL (equivalent to 1.82 mg/mL insulin) was added to the donor compartment, whereas the receptor compartment was filled with isotonic PBS (pH 7.4).…”

Section: Ex Vivo Permeability Studiesmentioning

confidence: 99%

Development, Characterization, and Ex Vivo Assessment of Elastic Liposomes for Enhancing the Buccal Delivery of Insulin

et al. 2021

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Buccal drug delivery is a suitable alternative to invasive routes of drug administration. The buccal administration of insulin for the management of diabetes has received substantial attention worldwide. The main aim of this study was to develop and characterize elastic liposomes and assess their permeability across porcine buccal tissues. Sodium-cholate-incorporated elastic liposomes (SC-EL) and sodium-glycodeoxycholate-incorporated elastic liposomes (SGDC-EL) were prepared using the thin-film hydration method. The prepared liposomes were characterized and their ex vivo permeability attributes were investigated. The distribution of the SC-EL and SGDC-EL across porcine buccal tissues was evaluated using confocal laser scanning microscopy (CLSM). The SGDC-EL were the most superior nanocarriers since they significantly enhanced the permeation of insulin across porcine buccal tissues, displaying a 4.33-fold increase in the permeability coefficient compared with the insulin solution. Compared with the SC-EL, the SGDC-EL were better at facilitating insulin permeability, with a 3.70-fold increase in the permeability coefficient across porcine buccal tissue. These findings were further corroborated based on bioimaging analysis using CLSM. SGDC-ELs showed the greatest fluorescence intensity in buccal tissues, as evidenced by the greater shift of fluorescence intensity toward the inner buccal tissue over time. The fluorescence intensity ranked as follows: SGDC-EL > SC-EL > FITC–insulin solution. Conclusively, this study highlighted the potential nanocarriers for enhancing the buccal permeability of insulin.

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Section: Ex Vivo Permeability Studiesmentioning

confidence: 99%

Development, Characterization, and Ex Vivo Assessment of Elastic Liposomes for Enhancing the Buccal Delivery of Insulin

et al. 2021

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“…Gelatin methacryloyl (GelMA) hydrogels were used as the matrix for the controlled release of 5-fluorouracil (Oktay & Alemdar, 2018 ). Polyvinyl alcohol and polyvinyl pyrrolidone (PVA-PVP) blended hydrogels were used as the matrix for the controlled release of donepezil hydrochloride (DH) (Bashyal et al., 2020 ).…”

Section: Introductionmentioning

confidence: 99%

Enhanced transdermal insulin basal release from silk fibroin (SF) hydrogels via iontophoresis

2022

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Insulin is the peptide hormone used to treat the diabetes patient. The hormone is normally taken by injection. The transdermal drug delivery system (TDDS) is an alternative route. The silk fibroin (SF) hydrogels were fabricated via solution casting as the insulin matrix. The release and release-permeation experiments of the insulin loaded SF hydrogels were carried out using a modified Franz-diffusion cell at 37 °C for 36 h, under the effects of SF concentrations, pH, and electric field. The release-permeation mechanism through the pig skin was from the Case-II transport with the constant release rate. The diffusion coefficient (D) increased with decreasing SF concentration due to a larger mesh size, and with increasing electric field due to the electroreplusive forces between the insulin and the SF hydrogels against the negatively-charged electrode, and the induced SF hydrogel expansion. The rate and amount of insulin release-permeation became relatively lower as it required a longer time to generate aqueous pathways through the pig skin. The present SF hydrogels are demonstrated here deliver insulin with the required constant release rate, and the suitable amount within a prescribed duration.

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“…In addition, hybridization of HSA significantly reduced the C max value, indicating the reduced initial burst release of DNP. There were several reports on the subcutaneous administration of DNP, including dual-crosslinked hydrogels and microneedle array patches [41][42][43]. However, we believe that hybridization of MLCs and HSA in an HA hydrogel is a novel approach that can achieve longer T max and lower C max values.…”

Section: Discussionmentioning

confidence: 93%

Subcutaneously Injectable Hyaluronic Acid Hydrogel for Sustained Release of Donepezil with Reduced Initial Burst Release: Effect of Hybridization of Microstructured Lipid Carriers and Albumin

et al. 2021

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The daily oral administration of acetylcholinesterase (AChE) inhibitors for Alzheimer’s disease features low patient compliance and can lead to low efficacy or high toxicity owing to irregular intake. Herein, we developed a subcutaneously injectable hyaluronic acid hydrogel (MLC/HSA hydrogel) hybridized with microstructured lipid carriers (MLCs) and human serum albumin (HSA) for the sustained release of donepezil (DNP) with reduced initial burst release. The lipid carrier was designed to have a microsized mean diameter (32.6 ± 12.8 µm) to be well-localized in the hydrogel. The hybridization of MLCs and HSA enhanced the structural integrity of the HA hydrogel, as demonstrated by the measurements of storage modulus (G′), loss modulus (G″), and viscosity. In the pharmacokinetic study, subcutaneous administration of MLC/HSA hydrogel in rats prolonged the release of DNP for up to seven days and reduced the initial plasma concentration, where the Cmax value was 0.3-fold lower than that of the control hydrogel without a significant change in the AUClast value. Histological analyses of the hydrogels supported their biocompatibility for subcutaneous injection. These results suggest that a new hybrid MLC/HSA hydrogel could be promising as a subcutaneously injectable controlled drug delivery system for the treatment of Alzheimer’s disease.

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Preparation, Characterization, and In Vivo Pharmacokinetic Evaluation of Polyvinyl Alcohol and Polyvinyl Pyrrolidone Blended Hydrogels for Transdermal Delivery of Donepezil HCl

Cited by 24 publications

References 48 publications

Development, Characterization, and Ex Vivo Assessment of Elastic Liposomes for Enhancing the Buccal Delivery of Insulin

Development, Characterization, and Ex Vivo Assessment of Elastic Liposomes for Enhancing the Buccal Delivery of Insulin

Enhanced transdermal insulin basal release from silk fibroin (SF) hydrogels via iontophoresis

Subcutaneously Injectable Hyaluronic Acid Hydrogel for Sustained Release of Donepezil with Reduced Initial Burst Release: Effect of Hybridization of Microstructured Lipid Carriers and Albumin

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