scholarly journals Topical Chitosan-Based Thermo-Responsive Scaffold Provides Dexketoprofen Trometamol Controlled Release for 24 h Use

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2100
Author(s):  
Luis Castillo-Henríquez ◽  
Pablo Sanabria-Espinoza ◽  
Brayan Murillo-Castillo ◽  
Gabriela Montes de Oca-Vásquez ◽  
Diego Batista-Menezes ◽  
...  

Chronic and non-healing wounds demand personalized and more effective therapies for treating complications and improving patient compliance. Concerning that, this work aims to develop a suitable chitosan-based thermo-responsive scaffold to provide 24 h controlled release of Dexketoprofen trometamol (DKT). Three formulation prototypes were developed using chitosan (F1), 2:1 chitosan: PVA (F2), and 1:1 chitosan:gelatin (F3). Compatibility tests were done by DSC, TG, and FT-IR. SEM was employed to examine the morphology of the surface and inner layers from the scaffolds. In vitro release studies were performed at 32 °C and 38 °C, and the profiles were later adjusted to different kinetic models for the best formulation. F3 showed the most controlled release of DKT at 32 °C for 24 h (77.75 ± 2.72%) and reduced the burst release in the initial 6 h (40.18 ± 1.00%). The formulation exhibited a lower critical solution temperature (LCST) at 34.96 °C, and due to this phase transition, an increased release was observed at 38 °C (88.52 ± 2.07% at 12 h). The release profile for this formulation fits with Hixson–Crowell and Korsmeyer–Peppas kinetic models at both temperatures. Therefore, the developed scaffold for DKT delivery performs adequate controlled release, thereby; it can potentially overcome adherence issues and complications in wound healing applications.

Author(s):  
Luis Castillo-Henríquez ◽  
Pablo Sanabria-Espinoza ◽  
Brayan Murillo-Castillo ◽  
Gabriela Montes de Oca- Vásquez ◽  
Diego Batista-Menezes ◽  
...  

Chronic and non-healing wounds demand personalized and more effective therapies for treating complications and improve patient adherence. This work aims to develop a suitable chitosan-based scaffold to provide 24 hours controlled release of DKT, by taking advantage of chitosan’s thermo-responsive behavior as well as local hyperthermia in wounds. Three formulation prototypes were developed using chitosan (F1), 2:1 chitosan: PVA (F2), and 1:1 chitosan:gelatin (F3). Compatibility tests were done by DSC, TG, and IR spectroscopy. SEM was employed to examine the morphology of the surface and inner layers from the scaffolds. In vitro release studies were performed at 32 °C and 38 °C to evaluate the release profiles, which were later adjusted to different kinetic models for the best formulation. F3 showed the most controlled release of DKT at 32 °C for 24 hours (77.75 ± 2.72 %), and reduced the burst release in the initial 6 hours (40.18 ± 1.00 %), while at 38 °C the release reached 88.52 ± 2.07 % at 12 hours. The release profile for this formulation fits with Hixson-Crowell and Korsmeyer-Peppas kinetic models at both temperatures. Therefore, the developed chitosan/gelatin thermo-responsive scaffold provides a suitable system for wound healing with a controlled release of DKT for 24 hour-use, which can overcome adherence issues and wound complications.


2021 ◽  
Vol 21 (11) ◽  
pp. 5723-5735
Author(s):  
Sofiya Shaikh ◽  
Hemil Patel ◽  
Debes Ray ◽  
Vinod K. Aswal ◽  
Rakesh K. Sharma

Recently the applications of Poloxamers in drug development is promising as it facilitated the drug molecule for delivering to the correct place, at the correct time and in the correct amount. Poloxamers can form nanomicelles to encapsulate hydrophobic drugs in order to increase solubility, stability and facilitate delivery at target. In this context, the solubilization of anticonvulsant lamotrigine (LMN) drug in a chain of Poloxamers containing different polyethylene oxide and polypropylene oxide noieties were examined. The results showed better solubilization of LMN in Poloxamers contain low CMTs while poor with Poloxamers having high CMTs. Systematic investigation of two mixed Poloxamer nanomicelles (P407:P403 and P407:P105) for LMN bioavailability at body temperature (37 °C) were investigated. The solubility of LMN was enhanced in mixed P407:P403 nanomicelles with the amount of P403 and reduced in mixed P407:P105 nanomicelles with the amount of P105. LMN encapsulated mixed Poloxamer nanomicelles were found spherical in shape with ~25 nm Dh sizes. The In-Vitro release profiles of mixed Poloxamer nanomicelles demonstrated the biphasic model with initial burst release and then slowly release of LMN. Better biocompatibility of LMN in the mixed P407:P403 nanomicelles was confirmed with stability data. The results of this work were proven the mixed P407:P403 nanomicelles as efficient nanocarriers for LMN.


2017 ◽  
Vol 1 (2) ◽  
pp. 01-04
Author(s):  
Saritha Garrepalli

Prepared nanoparticles were characterized in terms of particle size, scanning electron microscope (SEM), fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). In-vitro release studies were performed in phosphate buffer saline pH 7.4 at 37˚±0.5˚C for 1month. The mean particle size of obtained nanoparticles was 150-400 nm and was apparently spherical in shape, with smooth surface. DSC is done for the stability test for pure drug and sample. The thermogram of drug has not shifted for in the formulation compare to pure drug thermogram hence, the stability of formulation is not changed. FT-IR studies demonstrated that the drug was not changed in the formulation during the fabrication process.The encapsulation efficiency was about 48%. The Anastrozole-BSA nanoparticles exhibit a most interesting release profile with small initial burst followed by slower and controlled release.


1970 ◽  
Vol 5 (1) ◽  
pp. 33-37
Author(s):  
Md. Shamsuddin ◽  
Parvin Akter ◽  
Md. Ziaur Rahman Khan ◽  
Jakir Ahmed Chowdhury ◽  
Md. Selim Reza

Controlled release matrix tablets of theophylline anhydrous were designed with different types of bioadhesive polymers. HPMC 15 cps and 50 cps, Na-CMC, Gelatin, Xanthun gum and PVP K-30 were selected to formulate matrix tablets. Tablets of theophylline were prepared by direct compression method and were subjected to in vitro drug dissolution for 8 hrs in a gastric fluid media by using thermal shaker with a shaking speed of 50 rpm at a temperature of 37 ± 0.5°C. The in vitro release study as well as retention time of bioadhesive tablets on mucous membrane were investigated to develop a bioadhesive polymer based controlled release delivery system and to evaluate the performance of such delivery device. Na-CMC, HPMC and Xanthan gum based tablets showed greater bio-adhesive strength where as gelatin and PVP K-30 based tablets showed poor bioadhesive strength. Na-CMC and Xanthun gum loaded tablets were not discharged from the mucous membrane and these tablets were fully dissolved in the gastric fluid. Xanthan gum, Na-CMC and HPMC based formulation showed nearly zero-order release. On the contrary, gelatin and PVP K-30 based formulation showed a burst release within one hour of dissolution. Key words: Bio-adhesion, Release profile, theophylline anhydrous. Dhaka Univ. J. Pharm. Sci. Vol.5(1-2) 2006 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website


2020 ◽  
Vol 11 (6) ◽  
pp. 373-386
Author(s):  
Ishwor Poudel ◽  
Manjusha Annaji ◽  
Robert D Arnold ◽  
Amal Kaddoumi ◽  
Nima Shamsaei ◽  
...  

Aim: Additively manufactured (3D printed), stainless steel implants were coated with dexamethasone using gelatin, chondroitin sulfate for use in bone graft surgeries. Materials & methods: The drug and polymers were deposited on the implants with a rough surface using a high precision air brush. The gelatin-chondroitin sulfate layers were cross-linked using glutaraldehyde. Results: The drug content uniformity was within 100 ± 5%, and the thickness of the polymer layer was 410 ± 5.2 μm. The in vitro release studies showed a biphasic pattern with an initial burst release followed by slow release up to 3 days. Conclusion: These results are very promising as the slow release implants can be further tested in vivo in large animals, such as cattle and horses to prevent the inflammatory cascade following surgeries.


Polymers ◽  
2021 ◽  
Vol 13 (15) ◽  
pp. 2576
Author(s):  
Majid Abdouss ◽  
Nastaran Radgoudarzi ◽  
Alireza Mohebali ◽  
Elaheh Kowsari ◽  
Mojtaba Koosha ◽  
...  

In this study, a novel promising approach for the fabrication of Halloysite nanotube (HNT) nanocomposites, based on the amino acid named Methionine (Met), was investigated. For this purpose, Met layered on the outer silane functionalized surface of HNT for controlled release of Phenytoin sodium (PHT). The resulting nanocomposite (MNT-g-Met) was characterized by FTIR, XRD, Zeta potential, TGA, TEM and FE-SEM. The FT-IR results showed APTES and Met peaks, which proved the modification of the HNTs. The zeta-potential results showed the interaction between APTES (+53.30) and Met (+38.80) on the HNTs (−30.92). The FE-SEM micrographs have displayed the grafting of Met on the modified HNTs due to the nanotube conversion to a rough and indistinguishable form. The amount of encapsulation efficiency (EE) and loading efficiency (LE) of MNT-g-Met was 74.48% and 37.24%, while pure HNT was 57.5%, and 28.75%, respectively. In-vitro studies showed that HNT had a burst release (70% in 6 h) in phosphate buffer while MNT-g-Met has more controlled release profile (30.05 in 6 h) and it was found to be fitted with the Korsmeyer-Peppas model. Due to the loading efficiency and controlled release profile, the nanocomposite promote a good potential for drug delivery of PHT.


2019 ◽  
Vol 9 (4) ◽  
pp. 601-608 ◽  
Author(s):  
Hamid Rahmani ◽  
Ali Fattahi ◽  
Komail Sadrjavadi ◽  
Salar Khaledian ◽  
Yalda Shokoohinia

Purpose: The aim of this study is to prepare 5-fluorouracil (5-FU) loaded silk fibroin nanoparticles(SFNPs) and to achieve a controlled release delivery system with the high loading capacity. Methods: SFNPs with 1:1, 1:3, and 1:10 ratios of 5-FU to silk fibroin were prepared. SFNPswere characterized by Fourier-transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD)analysis, Scanning electron microscope (SEM), and Transmission electron microscope (TEM).Loading efficiency, in vitro release, and cell viability were studied for optimal SFNPs. Results: The ratio of 1:1 was optimal formulation with the size and polydispersity index (PDI)of 221.03 nm and 0.093 before freeze drying, and 286.7 nm and 0.154 after freeze dryingby lactose, respectively. The loading efficiency and loading content of this ratio were 52.32%and 34.35%, respectively. FT-IR and XRD analysis indicated the conformational change (fromrandom coil to β-sheet) in the structure of nanoparticles by increasing amount of the drug, whichcaused the smaller size, the higher loading efficiency, and the slower release pattern. The drugloadednanoparticles reached to the half maximal inhibitory concentration (IC50) that werecomparable with free drug on MCF7 (human breast cancer) cell line. Conclusion: This study was planned to achieve a promising controlled release drug deliverysystem for carrying 5-FU, as a potent anticancer drug. SFNPs were found proper candidates fordelivery of a hydrophilic drug such as 5-FU.


Author(s):  
Sharma K ◽  
Khan AD ◽  
Sachdeva M

The oral transmucosal Timolol maleate delivery bypasses liver and avoids presystemic elimination in the gastro intestinal tract andliver which enhance the bioavailability as well decreases the adverse effect. Objective: The present investigation highlights the formulation andevaluation of mucoadhesive buccal patch of Timolol maleate because Timolol maleate has biphasic solubility hence relatively permeated throughbuccal mucosa, which is well supplied with both vascular and lymphatic drainage. Material and Method: The mucoadhesive buccal patches ofTimolol maleate were prepared by solvent casting technique using polymers like Hydroxypropylmethyl cellulose-15cps and Polyvinylpyrrolidone. The formulated films were evaluated for their physiochemical parameters like surface pH, percentage moisture absorption, swellingpercentage, thickness, folding endurance and drug content. In vitro permeation and in vitro release studies were performed with pH 6.8 phosphatebuffer solution. Result and Discussion: The patches exhibited controlled release for more than 12 h. The in vitro release data were fit to differentequations and kinetic models to explain release profiles. The kinetic models used were zero order, first order higuchi’s and peppa’s. The bestmucoadhesive performance and matrix controlled release was exhibited by the formulation CK2 (3 % HPMC and 1 % PVP). Conclusion: Goodresults were obtained both in physico chemical characteristics and in vitro studies in formulation CK2. Hence the formulations of Timololmaleate bioadhesive buccal patch is a promising one as the controlled drug delivery with improved bioavailability.


Author(s):  
Mashkura Ashrafi ◽  
Jakir Ahmed Chowdhury ◽  
Md Selim Reza

Capsules of different formulations were prepared by using a hydrophilic polymer, xanthan gum and a filler Ludipress. Metformin hydrochloride, which is an anti-diabetic agent, was used as a model drug here with the aim to formulate sustained release capsules. In the first 6 formulations, metformin hydrochloride and xanthan gum were used in different ratio. Later, Ludipress was added to the formulations in a percentage of 8% to 41%. The total procedure was carried out by physical mixing of the ingredients and filling in capsule shells of size ‘1’. As metformin hydrochloride is a highly water soluble drug, the dissolution test was done in 250 ml distilled water in a thermal shaker (Memmert) with a shaking speed of 50 rpm at 370C &plusmn 0.50C for 6 hours. After the dissolution, the data were treated with different kinetic models. The results found from the graphs and data show that the formulations follow the Higuchian release pattern as they showed correlation coefficients greater than 0.99 and the sustaining effect of the formulations was very high when the xanthan gum was used in a very high ratio with the drug. It was also investigated that the Ludipress extended the sustaining effect of the formulation to some extent. But after a certain period, Ludipress did not show any significant effect as the pores made by the xanthan gum network were already blocked. It is found here that when the metformin hydrochloride and the xanthan gum ratio was 1:1, showed a high percentage of drug release, i.e. 91.80% of drug was released after 6 hours. But With a xanthan gum and metformin hydrochloride ratio of 6:1, a very slow release of the drug was obtained. Only 66.68% of the drug was released after 6 hours. The percent loading in this case was 14%. Again, when Ludipress was used in high ratio, it was found to retard the release rate more prominently. Key words: Metformin Hydrochloride, Xanthan Gum, Controlled release capsule Dhaka Univ. J. Pharm. Sci. Vol.4(1) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website


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