scholarly journals Electrospun PVP/PVA Nanofiber Mat as a Novel Potential Transdermal Drug-Delivery System for Buprenorphine: A Solution Needed for Pain Management

2021 ◽  
Vol 11 (6) ◽  
pp. 2779
Author(s):  
Fatemeh Rahmani ◽  
Hakimeh Ziyadi ◽  
Mitra Baghali ◽  
Hongrong Luo ◽  
Seeram Ramakrishna

Over the past several decades, the formulation of novel nanofiber-based drug-delivery systems has been a frequent focus of scientists around the world. Aiming to introduce a novel nanofibrous transdermal drug-delivery system to treat pain, the nanofiber mats of buprenorphine-loaded poly (vinyl pyrrolidone) (Bup/PVP) and buprenorphine-loaded poly(vinyl alcohol)/poly(vinyl pyrrolidone) (Bup/PVP/PVA) were successfully fabricated by the electrospinning process for transdermal drug delivery. Similarly, PVP and PVP/PVA nanofibers were fabricated in the same conditions for comparison. The viscosity and electrical conductivity of all electrospinning solutions were measured, and nanofiber mats were characterized by scanning electron microscopy (SEM), atomic force microscopy (AFM), Fourier transform infrared (FT-IR) spectroscopy and contact angle analysis. The conductivity of PVP and PVP/PVA solutions showed a considerable increase by the addition of buprenorphine due to the polarity of buprenorphine. SEM images showed a smooth, fine and porous nanofibrous structure without any adhesion or knot for all of the samples. The contact angle analysis showed the increased hydrophilicity and wettability of PVP/PVA and Bup/PVP/PVA nanofibers compared to PVP and Bup/PVP nanofibers which can be attributed to the addition of PVA. Attenuated total reflectance (ATR) FT-IR results confirmed that the electrospinning process did not affect the chemical integrity of the drug. For the modification of the drug release rate, the cross-linking of nanofiber mats was carried out using glutaraldehyde. Drug release measurements using high-performance liquid chromatography (HPLC) analysis demonstrated that Bup/PVP/PVA nanofibers exhibited better physical and chemical properties compared to Bup/PVP. Furthermore, the cross-linking of nanofibers led to an increase in drug release time. Thus, the novel buprenorphine-loaded nanofibers can be efficient biomaterial patches for transdermal delivery against pain improving carrier retention and providing a controlled release of the drug.

2018 ◽  
Vol 10 (1) ◽  
pp. 67
Author(s):  
Bhawana Sethi ◽  
Rupa Mazumder

Objective: The present work was aimed at preparation of transdermal patches by a solvent casting method using a varying concentration of polymers i.e. methocel (K15 and K100), ethocel (4 and 10), gelatin, chitosan, eudragit (RL and RS) grade using plasticizer (glycerin and propylene glycol).Methods: The ratio of drug to polymers and plasticizer was varied and the effect of formulation variables was studied. Prepared transdermal patches were evaluated for physicochemical properties, in-vitro permeation studies, content uniformity, primary skin irritation studies and FT-IR studies.Results: The formulated transdermal patch by using Methocel K 100 M showed good physical properties. The average weight of patches prepared using glycerin as a plasticizer were ranged from 42.33-67.00 mg and propylene glycol as a plasticizer were ranged from 40.67-67.67 mg. The percentage moisture absorption varies from 1.76 to 10.73 for patches formulated using glycerin and 2.28 to 7.97 for propylene glycol patches. The percentage moisture loss from patches prepared using glycerin was ranged from 2.75 to 11.54 and 2.87 to 12.02 from propylene glycol. The water vapour transmission rate from patches prepared using glycerin was ranged from 0.25 to 0.92 and 0.41 to 1.76. The formulated patch showed the acceptable quantity of medicament ranged from (100.20-101.05%). This result met the test content uniformity as per BP (85% to 115%). According to that, the drug was consistent throughout the patches. The formulation PGD is considered as the best formulation, since it shows a maximum in vitro drug release as 43.75 % at 24 h. The drug release kinetics studied showed that the majority of formulations was following zero order.Conclusion: In conclusion, controlled release transdermal drug delivery system patches of aliskiren can be prepared using polymer combinations, with a different plasticizer. The release rate of drug depends upon the polymer. However, release kinetics followed zero order.


Author(s):  
DIPJYOTI BISWAS ◽  
SUDIP DAS ◽  
SOURAV MOHANTO ◽  
SHUBHRAJIT MANTRY

The modified/regulated drug delivery system helps to sustain the delivery of the drug for a prolonged period. The modified drug delivery system is primarily aimed at ensuring protection, the effectiveness of the drug, and patient compliance. The transdermal drug delivery system (TDDS) falls within the modified drug delivery system, in which the goal is to deliver the drug at a fixed dose and regulated rate through the skin. Polymers are the backbone of the framework for providing transdermal systems. The polymer should be stable, non-toxic, economical, and provide a sustainable release of the drug. In general, natural polymers used in the TDDS as rate-controlling agents, protective, and stabilizing agents and also used to minimize the frequency of dosing and improve the drug’s effectiveness by localizing at the site of action. Nowadays, manufacturers are likely to use natural polymers due to many issues associated with drug release and side effects with synthetic polymers. Drug release processes from natural polymers include oxidation, diffusion, and swelling. Natural polymers may be used as the basis to achieve predetermined drug distribution throughout the body. The use of natural materials for traditional and modern types of dosage forms are gums, mucilages, resins, and plant waste etc. Thus, the main objective of this review article is to give a brief knowledge about the extraction, modification, characterization, and biomedical application of conventional natural polymers used in the transdermal drug delivery system and their future prospective.


Author(s):  
Subramanian S ◽  
Senith SK

Transdermal drug delivery is an alternative route for systemic drug delivery which minimizes the absorption and increases the bioavailability. Orally clopidogrel bisulfate has a short elimination half-life (7-8 h), low oral bioavailability (50 %) undergoes extensive first pass metabolism (85 %) and frequent high doses (75 mg) are required to maintain the therapeutic level as a result. The purpose of this research was formulation and evaluation of transdermal drug delivery system of clopidogrel bisulfate using various polymers such as HPMC and EC by solvent casting technique for improvement of bioavailability of drug and reducing toxic effects. The developed transdermal patches may increase the therapeutic efficacy and reduce toxic effect of clopidogrel bisulfate. The prepared transdermal drug delivery system of clopidogrel bisulfate using different polymers such as HPMC and EC had shown good & promising results for all the evaluated parameters. Based on the in vitro drug release, drug content, weight variation, tensile strength, thickness and folding endurance results formulation F2 was concluded as an optimized formulation which shows its higher percentage of drug release. Keyword: Clopidogrel bisulfate; Transdermal patch; TDDS; Solvent evaporation; In vitro drug release


Author(s):  
Karishma Tole ◽  
Ganesh Deshmukh

Objective: The objective was to improve the bioavailability, stability of formulation, and skin permeability of Duloxetine HCl.Method: Microemulsion was prepared with oleic acid as oil, water, and Smix ratio of tween 20 to propylene glycol (1:3). Pseudo-ternary phase diagrams were constructed to determine the region of existence of microemulsions prepared using oil titration method. Optimization of formulations was done based on the in vitro diffusion studies. The microemulsion was gelled using carbopol 934p and HPMCK 100 as the gelling agent.Result: After the analysis of different evaluation parameter and drug release, the F3 batch was selected as a promising formulation for delivery of duloxetine HCl as a microemulsion gel for transdermal drug delivery with 79.607% drug release in 10 h.Conclusion: It was observed that transdermal microemulsion gel can be formulated successfully for duloxetine HCl with improved bioavailability. Among the other batches, the F3 batch was selected as an optimized batch because all the evaluation parameters results are satisfactory. From stability data, the formulation was found to be stable as no phase separation or turbidity was observed in the formulation after 3 months.


Author(s):  
P. Srikanth Reddy ◽  
V. Alagarsamy ◽  
G. Ravi ◽  
P. Subhash Chandra Bose ◽  
D. Saritha

Transdermal drug delivery is an alternative route for systemic drug delivery which minimizes the absorption and increases the bioavailability. The main objective of the present work was to develop a suitable matrix type transdermal drug delivery system of Clopidogrel bisulphate using different polymers HPMC E15, Eudragit L100 and to compare the drug release through physical method and chemical method. Matrix type transdermal patches containing Clopidogrel Bisulfate were prepared by solvent evaporation technique. The prepared transdermal patches were evaluated for Thickness, folding endurance, tensile strength and in vitro studies. The prepared transdermal drug delivery system of Clopidogrel bisulphate using different polymers such as HPMC E15 and Eudragit L 100 had shown good promising results for all the evaluated parameters. Based on the In-vitro drug release, drug content and folding endurance results formulation F4 was concluded as an optimized formulation which shows its higher percentage of drug release. Keywords: Transdermal drug delivery, Clopidogrel bisulphate, HPMC E15, Eudragit L100


2011 ◽  
Vol 2011 ◽  
pp. 1-9 ◽  
Author(s):  
Sureewan Duangjit ◽  
Praneet Opanasopit ◽  
Theerasak Rojanarata ◽  
Tanasait Ngawhirunpat

The goal of this study was to develop and evaluate the potential use of liposome and transfersome vesicles in the transdermal drug delivery of meloxicam (MX). MX-loaded vesicles were prepared and evaluated for particle size, zeta potential, entrapment efficiency (%EE), loading efficiency, stability, and in vitro skin permeation. The vesicles were spherical in structure, 90 to 140 nm in size, and negatively charged ( to  mV). The %EE of MX in the vesicles ranged from 40 to 70%. Transfersomes provided a significantly higher skin permeation of MX compared to liposomes. Fourier Transform Infrared Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC) analysis indicated that the application of transfersomes significantly disrupted the stratum corneum lipid. Our research suggests that MX-loaded transfersomes can be potentially used as a transdermal drug delivery system.


2011 ◽  
Vol 338 ◽  
pp. 42-45 ◽  
Author(s):  
Tanasait Ngawhirunpat ◽  
Theerasak Rojanarata ◽  
Suwannee Panomsuk ◽  
Praneet Opanasopit

The aim of this study was to prepare and characterize electrospun polyvinyl alcohol (PVA) nanofiber mats loaded with capsaicin (CC) as a transdermal drug delivery system. The amount of CC loaded in the base PVA solution (10 %w/v solution) was 0.025, 0.0375 and 0.05 %, based on the dry weight of PVA (% wt). The average diameters of these fibers ranged from 121 to 165 nm. In all concentrations of CC loaded in spun PVA fiber mats, an amorphous nanodispersion of CC with PVA was obtained. The tensile strength of the as-spun fiber mats was lower than that of the as-cast PVA films. The release rate of CC from CC-loaded as-spun PVA was significantly higher than from CC-loaded as-cast PVA films, and increased when the CC content in both CC-loaded as-spun PVA and CC-loaded as-cast PVA films increased. Our research suggests a potential use for CC-loaded electrospun PVA mats as a transdermal drug delivery system.


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