scholarly journals Thermosensitive Drug Delivery System SBA-15-PEI for Controlled Release of Nonsteroidal Anti-Inflammatory Drug Diclofenac Sodium Salt: A Comparative Study

Materials ◽  
2021 ◽  
Vol 14 (8) ◽  
pp. 1880
Author(s):  
Lubos Zauska ◽  
Stefan Bova ◽  
Eva Benova ◽  
Jozef Bednarcik ◽  
Matej Balaz ◽  
...  

Mesoporous SBA-15 silica material was prepared by the sol–gel method and functionalized with thermosensitive polyethylenimine polymers with different molecular weight (g·mol−1): 800 (SBA-15(C)-800), 1300 (SBA-15(C)-1300) and 2000 (SBA-15(C)-2000). The nonsteroidal anti-inflammatory drug (NSAID) diclofenac sodium was selected as a model drug and encapsulated into the pores of prepared supports. Materials were characterized by the combination of infrared spectroscopy (IR), atomic force microscopy (AFM), transmission electron microscopy (TEM), photon cross-correlation spectroscopy (PCCS), nitrogen adsorption/desorption analysis, thermogravimetry (TG), differential scanning calorimetry (DSC) and small-angle X-ray diffraction (SA-XRD) experiments. The drug release from prepared matrixes was realized in two model media differing in pH, namely small intestine environment/simulated body fluid (pH = 7.4) and simulated gastric fluid (pH = 2), and at different temperatures, namely normal body temperature (T = 37 °C) and inflammatory temperature (T = 42 °C). The process of drug loading into the pores of prepared materials from the diclofenac sodium salt solutions with different concentrations and subsequent quantitative determination of released drugs was analyzed by UV-VIS spectroscopy. Analysis of prepared SBA-15 materials modified with polyethylenimines in solution showed a high ability to store large amounts of the drug, up to 230 wt.%. Experimental results showed their high drug release into the solution at pH = 7.4 for both temperatures, which is related to the high solubility of diclofenac sodium in a slightly alkaline environment. At pH = 2, a difference in drug release rate was observed between both temperatures. Indeed, at a higher temperature, the release rates and the amount of released drug were 2–3 times higher than those observed at a lower temperature. Different kinetic models were used to fit the obtained drug release data to determine the drug release rate and its release mechanism. Moreover, the drug release properties of prepared compounds were compared to a commercially available medicament under the same experimental conditions.

2012 ◽  
Vol 1 (7) ◽  
pp. 165-170 ◽  
Author(s):  
P V Swamy ◽  
Mohammed Younus Ali ◽  
Y Anand Kumar ◽  
K Prasad ◽  
N Srinivaslu

The aim of the present study was to design and evaluate the suppositories of aceclofenac a non-steroidal anti inflammatory drug (NSAID). Aceclofenac, rectal suppositories were developed by employing various hydrophilic and hydrophobic polymeric bases like gelatin, PEG-400 and hydrogenated vegetable oil using propylene glycol as plasticizer and beeswax as hardening agent. The in-vitro release rate data was evaluated statistically and was found that from all the formulations the drug release is by diffusion mechanism (r = 0.9547 to 0.9967) according to Higuchi’s equation. All the prepared formulations have shown zero-order release kinetics except those prepared by utilizing 15% and 20 % of PEG-400. The formulation prepared using 7.5% beeswax in hydrogenated vegetable oil has displayed zero-order drug release (r = 0.9927) and has released 99.18% of the aceclofenac within 4h, hence, this formulation is considered as a promising formulation. The stability study on the promising formulation was conducted over a period of 6 months and found that there are no significant changes in the drug content and in-vitro drug release rate (p<0.05). The result suggests that the suppositories can be prepared by employing hydrophilic and hydrophobic polymers.DOI: http://dx.doi.org/10.3329/icpj.v1i7.10810International Current Pharmaceutical Journal 2012, 1(7): 165-170


2020 ◽  
Vol 2020 ◽  
pp. 1-19
Author(s):  
Desta Tesfay ◽  
Solomon Abrha ◽  
Zewdu Yilma ◽  
Gebremariam Woldu ◽  
Fantahun Molla

Ensete ventricosum (Welw.) cheeseman which belongs to the family of Musaceae is one of the main sources of starch in Ethiopia. This study aimed at evaluating epichlorohydrin cross-linked enset starch as a drug release sustaining excipient in microsphere formulations of theophylline. Extracted enset starch was cross-linked using epichlorohydrin as a cross-linking agent. The effect of cross-linker concentration, cross-linking duration, and cross-linking temperature on the degree of cross-linking and release rate of microspheres prepared by emulsion solvent evaporation method was investigated using the two-level full factorial design. Accordingly, the concentration of epichlorohydrin and duration of cross-linking were the most significant factors affecting both the degree of cross-linking and drug release rate. Thus, the effects of these two factors were further studied and optimized using the central composite design. As per the numerical method of central composite design, the optimal points were obtained at epichlorohydrin concentration of 13.70% and cross-linking time of 3.82 h. Under these optimal conditions, the model predicts the degree of cross-linking of 74.70% and drug release rate of 28.00 h1/2. The validity of these optimal points was confirmed experimentally. The microspheres of the optimum formulation also exhibited minimum burst release with sustained release for 12 h. Besides, the optimized formulation followed the Higuchi square root kinetic model with non-Fickian diffusion release mechanism. The finding of this study suggested that cross-linked enset starch can be used as an alternative drug-release-sustaining pharmaceutical excipient in microsphere formulation.


RSC Advances ◽  
2015 ◽  
Vol 5 (32) ◽  
pp. 25164-25170 ◽  
Author(s):  
Bo Zhang ◽  
Teng Zhang ◽  
Quanxi Wang ◽  
Tianrui Ren

A controlled release system was prepared, it based on UF modified PCC cells in which TEB are loaded into cells. It can control the drug release rate, depress the initial “burst effect”, and was efficacious in controlling wheat powdery mildew.


Biomaterials ◽  
2001 ◽  
Vol 22 (21) ◽  
pp. 2857-2865 ◽  
Author(s):  
Giacomo Fontana ◽  
Mariano Licciardi ◽  
Silvana Mansueto ◽  
Domenico Schillaci ◽  
Gaetano Giammona

Author(s):  
DHARMENDER PALLERLA ◽  
SUMAN BANOTH ◽  
SUNKARI JYOTHI

Objective: The objective of this study was to formulate and evaluate the Curcumin (CUR) encapsulated sodium alginate (SA)/badam gum (BG)/kaolin (KA) microbeads for controlled drug release studies. Methods: The fabricated microbeads were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (X-RD), and scanning electron microscopy (SEM). Dynamic swelling studies and in vitro release kinetics were performed in simulated intestinal fluid (pH 7.4) and simulated gastric fluid (pH 1.2) at 37 °C. Results: FTIR confirms the formation of microbeads. DSC studies confirm the polymorphism of CUR in drug loaded microbeads which indicate the molecular level dispersion of the drug in the microbeads. SEM studies confirmed the microbeads are spherical in shape with wrinkled and rough surfaces. XRD studies reveal the molecular dispersion of CUR and the presence of KA in the developed microbeads. In vitro release studies and swelling studies depend on the pH of test media, which might be suitable for intestinal drug delivery. The % of drug release values fit into the Korsmeyer-Peppas equation and n values are obtained in the range of 0.577-0.664, which indicates that the developed microbeads follow the non-Fickian diffusion drug release mechanism. Conclusion: The results concluded that the CUR encapsulated microbeads are potentially good carriers for controlled drug release studies.


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