Graphene oxide as a functional excipient in buccal films for delivery of clotrimazole: Effect of molecular interactions on drug release and antifungal activity in vitro

2020 ◽  
Vol 589 ◽  
pp. 119811 ◽  
Author(s):  
J. Huang ◽  
J. Jacobsen ◽  
S.W. Larsen ◽  
N. Genina ◽  
M. van de Weert ◽  
...  
Keyword(s):  
Graphene Oxide ◽  
Antifungal Activity ◽  
Drug Release ◽  
Molecular Interactions ◽  
Buccal Films

Development and Evaluation of Trans Buccal Patches based on Natural and Synthetic Polymers Loaded with Rivastigmine using Solvent Casting Technique

2021 ◽  
pp. 5133-5140
Author(s):  
Prasanta Kumar Mohapatra ◽  
Boddu Pavan Kumar ◽  
Pankaj Singh Patel ◽  
Harish Chandra Verma ◽  
Satyajit Sahoo
Keyword(s):  
Drug Release ◽  
Kinetic Equations ◽  
Moisture Loss ◽  
Release Mechanism ◽  
Solvent Casting ◽  
Casting Technique ◽  
Weight Variation ◽  
Zero Order Release ◽  
Buccal Films

Mucoadhesive buccal films of rivastigmine were prepared by the solvent casting technique using HPMC K15M, sodium alginate, glycerine, and Eudragit RL100. Arranged films assessed for weight variation, thickness, % drug substance, % moisture loss, % moisture take-up, folding endurance, in-vitro medicament release, and Fourier transform Infrared spectroscopy (FTIR). The films showed a controlled release (CR) over 8 h. The preparation observed to be a worthy candidate for the development of buccal patches for therapeutic purposes. Drug-polymer compatibility considers FTIR demonstrated no contradiction between the medicament and the polymers. The optimized formulation found F7 indicated drug release 85% at the end of 8 h. Thinking about the correlation coefficient (R2) values got from the kinetic equations, the drug release from the formulations F1-F8 has discovered zero-order release mechanism. It can be concluded that oral buccal patches of rivastigmine, for treatment of Alzheimer’s and Parkinson’s disease, can be formulated. The study suggests that rivastigmine can be conveniently administered orally in the form of buccal patches, with the lesser occurrence of its side effects and improved bioavailability.

Development of Nateglinide Loaded Graphene Oxide-Chitosan Nanocomposites: Optimization by Box Behnken Design

2019 ◽  
Vol 11 (2) ◽  
pp. 142-153
Author(s):  
Rutuja V. Deshmukh ◽  
Pavan Paraskar ◽  
S. Mishra ◽  
Jitendra Naik
Keyword(s):  
Fourier Transform ◽  
Graphene Oxide ◽  
Electron Microscope ◽  
Drug Release ◽  
Sustained Release ◽  
Encapsulation Efficiency ◽  
In Vitro Drug Release ◽  
Box Behnken Design ◽  
X Ray

Background: Nateglinide is an antidiabetic drug having biological half-life 1.5 h which shows a concise effect. Graphene oxide along with chitosan can be used as a nanocarrier for sustained release of Nateglinide. Objective: To develop Nateglinide loaded graphene oxide-chitosan nanocomposites and to evaluate for different characterization studies. Methods: Graphene Oxide (GO) was synthesized by improved hummer’s method and drug-loaded Graphene oxide - chitosan nanocomposites were prepared. Box Behnken design was used to carry out experiments. The nanocomposites were characterized for encapsulation efficiency and drug release. Morphology was studied using field emission scanning electron microscope and transmission electron microscope. An interaction between drug, polymer and GO was investigated by Fourier transform infrared spectroscopy and X-ray diffractometer along with in vitro drug release study. Results: The statistical evaluation of the design showed linear and quadratic models which are significant models for encapsulation efficiency (R1 0.6883, 0.9473) and drug loading (R2 0.6785, 0.9336), respectively. Fourier transform infrared spectroscopy showed the compatibility of GO, Chitosan and Nateglinide. X-ray diffractometer reveals the change in degree of crystallinity of drug. FE-SEM and TEM images confirmed the distribution of the drug within the nanocomposites. Design expert reveals that the concentration of GO has great influence on encapsulation efficiency. In Vitro drug release showed the sustained release of drug over the period of 12 h. Conclusion: GO-Chitosan nanocomposites can be used as a sustained release carrier system for Nateglinide to reduce dose frequency of drug as well as its probable side effects.

A spatiotemporal anticancer drug release platform of PEGylated graphene oxide triggered by glutathione in vitro and in vivo

2012 ◽  
Vol 22 (45) ◽  
pp. 23845 ◽  
Author(s):  
Uuriintuya Dembereldorj ◽  
Mira Kim ◽  
Semi Kim ◽  
Erdene-Ochir Ganbold ◽  
So Yeong Lee ◽  
...  
Keyword(s):  
Graphene Oxide ◽  
Drug Release ◽  
Anticancer Drug

scholarly journals Characterization of bilayered matrix-type mucoadhesive buccal films containing tizanidine hydrochloride and piroxicam

2021 ◽  
Vol 20 (11) ◽  
pp. 2241-2248
Author(s):  
M. Yasmin Begum ◽  
Ali Alqahtani
Keyword(s):  
Drug Release ◽  
Patient Compliance ◽  
Residence Time ◽  
Ex Vivo ◽  
Drug Bioavailability ◽  
In Vitro Drug Release ◽  
Surface Ph ◽  
Folding Endurance ◽  
Buccal Films

Purpose: To formulate and characterize tizanidine hydrochloride (TZN) and piroxicam (PRX)-loaded bilayer mucoadhesive buccal films with an intention to improve the bioavailability and patient compliance in pain management.Methods: Bilayer buccal films were prepared by solvent evaporation technique using hydroxypropyl methylcellulose (HPMC) 15cps and polyvinylpyrrolidone (PVP K30 as immediate release (IR) layer forming polymers and HPMC K15 M, PVP K 90 along with various muco adhesive polymers (Carbopol P934, sodium alginate, etc), as sustained release (SR) layer forming polymers. The prepared films werecharacterized for thickness, weight variation, folding endurance, surface pH, swelling index,mucoadhesive strength, in vitro residence time, in vitro drug release, ex vivo permeation and drug release kinetics.Results: The prepared films were of largely uniform thickness, weight and drug content. Moisture loss (%) and folding endurance were satisfactory. Surface pH was compatible with salivary fluid. Disintegration time was 85 s for F1 and 115 s for F2 of IR films. In vitro dissolution studies showed 99.12 ± 1.2 % (F1) and 90.36 ± 1.8 % (F2) were released in 45 min. Based on the above results, F1 was chosen as the optimum formulation to be combined with SR layer of TZN. Amongst the SR layers of TZN in vitro drug release. The findings show that of F2 was 98.38 ± 0.82 % and correlated with ex vivo release. Drug release followed zero order release kinetics and mechanism of drug release was non-Fickian type diffusion. In vitro residence time was greater than 5 h.Conclusion: The findings show that the bilayer buccal films demonstrate the dual impact of deliveringPRX instantly from the IR layer, with good controlled release and permeation of TZN from the SR layer, thus providing enhanced therapeutic efficacy, drug bioavailability and patient compliance.

Unidirectional drug release from 3D printed mucoadhesive buccal films using FDM technology: In vitro and ex vivo evaluation

2019 ◽  
Vol 144 ◽  
pp. 180-192 ◽  
Author(s):  
Georgios K. Eleftheriadis ◽  
Christos Ritzoulis ◽  
Nikolaos Bouropoulos ◽  
Dimitrios Tzetzis ◽  
Dimitrios A. Andreadis ◽  
...  
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
3D Printed ◽  
Buccal Films

DESIGN AND IN VITRO EVALUATION OF MUCOADHESIVE BUCCAL FILMS OF LERCANIDIPINE HCL

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (07) ◽  
pp. 31-40
Author(s):  
H. Doddayya ◽  
◽  
S.S Patil ◽  
M Suman ◽  
P Kumar ◽  
...  
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Dsc Studies ◽  
Zero Order Kinetics ◽  
Accelerated Stability ◽  
Buccal Films ◽  
Lercanidipine Hydrochloride

Lercanidipine hydrochloride, an anti hypertension drug, undergoes extensive first pass metabolism to inactive metabolites leading to very poor oral bioavailability. To overcome this problem, buccal films of Lercanidipine hydrochloride were prepared by solvent casting method, employing HPMC, HPC (alone and in combination with PVP) and PVP K30. The film thickness, weight, folding endurance, mucoadhesive strength and time were dependent on the nature and concentration of polymers used. The optimized film (F12, HPMC 3% and PVP 1.5%) showed: Swelling index (51.26 ± 1.90 %), ex vivo mucoadhesive strength (12.64 ± 0.83 grams) and time (3.6 ± 0.5hrs). In vitro drug release was inversely proportional to the polymeric concentration. Ex- vivo drug release studies carried out using goat buccal membrane was slower (42.90%, 6 hrs) compared to in vitro drug release (74.2%, 8hrs) for the same formulation (F12). The drug release mechanism for the optimized formulation followed zero order kinetics. FT-IR and DSC studies revealed the absence of any interaction between the formulation ingredients. The films remained stable during the accelerated stability conditions.

Preparation, characterizations and in vitro evaluation of Econazole-Btamethasone loaded solid lipid nanoparticles (SLNs)

2021 ◽  
pp. 1-12
Author(s):  
Kamran Khan ◽  
Shefaat Ullah Shah ◽  
Yusuf S. Althobaithi ◽  
Kifayat Ullah Shah ◽  
Aman Ullah ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Side Effects ◽  
Drug Release ◽  
Oral Delivery ◽  
Encapsulation Efficiency ◽  
Fungal Infections ◽  
Ex Vivo ◽  
Sem Images ◽  
Drug Content

Tremendous increase of fungal infections in hospitalized or immune compromised patients has been reported from the last two decades. These infections are commonly treated using econazole and miconazole that have shorter half-life and produce severe side effects. All such issues can be addressed using targeted drug delivery. We developed SNLs based formulation for the treatment of mycosis. The high pressure homogenization method was employed for formulation followed by characterization, assay for antifungal activity, in vitro drug release and ex vivo permeation. The particle size of Econazole-Betamethasone-loaded SLNs, Econazole-loaded SLNs, Betamethasone-loaded SLNs and Blank SLNs were 377.4±23 nm, 298.7±9 nm, 177.7±15 nm and 113.4±6 nm respectively. The SEM images displayed that droplets are uniform and spherical in shape which ranged from 113.4±6 to 377.4±23 nm. In DSC, the SLNs formulation showed endothermic peak at 185.2 °C±0.9. Drug content of Econazole loaded SLNs was 82±0.1 and its entrapment efficiency was approximately 90.4±0.2. Betamethasone SLNs displayed highest drug content which was 83.5±0.4 while encapsulation efficiency of same formulation was 94.2±0.4. The Econazole and Betamethasone combined SLNs exhibited drug content of 80±0.3 while its encapsulation efficiency was 93.1±0.5. E-SLNs have significantly high drug release (p <  0.05) as compared to other formulation B-SLNs and EB-SLNs.The Econazole loaded formulations displayed antifungal activity with no synergistic or antagonistic effect with each other. Drug permeation from Econazole SLNs, Betamethasone SLNs and combined Econazole and Betamethasone SLNs was 45%, 40% and 38% respectively. Overall, SLN’s are an effective carrier for topical delivery of antifungals agents and that may be helpful in bypassing the serious side effects associated with oral delivery.

DESIGN OF PRONIOSOMAL GEL CONTAINING EUGENOL AS AN ANTIFUNGAL AGENT FOR THE TREATMENT OF ORAL CANDIDIASIS

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (09) ◽  
pp. 55-57
Author(s):  
T. S Vishnu ◽  
◽  
A. Dubey ◽  
G.S Ravi ◽  
S. Hebbar
Keyword(s):  
Antifungal Activity ◽  
Drug Release ◽  
Release Kinetics ◽  
Oral Candidiasis ◽  
In Vivo Studies ◽  
Compatibility Study ◽  
In Vitro Drug Release ◽  
Release Study

The objective of this study was to design and investigate the antifungal activity of proniosomal gel of eugenol for the treatment of oral candidiasis. The proniosomal gel was prepared by coacervation phase separation method using different surfactants like spans 20, 60, 80, soya lecithin and cholesterol. The proniosomal gel formulations were evaluated for visual inspection, pH detection, viscosity, spreadability, in vitro drug release and kinetics study, and in vivo studies. The compatibility study indicated that the drug and the excipients were compatible with each other. The results showed that pH, viscosity and spreadability were all acceptable for topical preparation. In vitro drug release study and drug release kinetics were conducted to check the release study and drug release patterns of the formulation. Amongst the formulations, an optimized formulation was selected to conduct an in vivo study. Candida albicans was used to induce oral candidiasis for the evaluation of therapeutic efficacy of proniosomal gel in immunosuppressed rats. Activity was analysed by microbiological and histopathological techniques and was compared with the marketed product. It is evident from the study that the proniosomal gel shows sustained release trend with strong antifungal activity.

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