scholarly journals Performance of HDTMA-Br-Modified Indonesian Zeolite as a Drug Carrier Candidate for Diclofenac Sodium

2021 ◽  
Vol 24 (3) ◽  
pp. 91-100
Author(s):  
Khafidhotun Naimah ◽  
Harjono Harjono ◽  
Jumaeri Jumaeri ◽  
Sri Kadarwati

Diclofenac sodium is a non-steroidal anti-inflammatory drug with a relatively short release time. This short release time promotes a more frequent drug consumption and could lead to side effects in the stomach, e.g., gastrointestinal disorders, gastrointestinal bleeding, and gastric ulcers. A drug delivery system with a slow-release activity is one of the promising technologies to control the drug amount released to the stomach. A surfactant-modified natural zeolite as a carrier for diclofenac sodium has been used in this study. This study focused on the preparation, characterization, and slow-release performance of HDTMA-modified natural zeolite as a carrier for diclofenac sodium. The zeolite underwent chemical and physical activation, as well as milling prior to use. It was proven that the zeolite used was dominated by mordenite and clinoptilolite with high stability properties towards acid treatments, as indicated by the XRD patterns. A modification of the zeolite surface using HDTMABr was also successfully performed, indicated by the appearance of peaks at wavenumbers of 2923.05 cm-1 and 2853.39 cm-1 (symmetrical and asymmetrical CH2 strains of HDTMA molecules, respectively) in the FTIR spectra. The synthesized HDTMA-modified natural zeolite also showed an excellent surface property such as surface area, pore-volume, and size, as indicated by the BET-BJH isotherms on the nitrogen adsorption. The slow-release performance of the zeolite-based drug delivery system was studied by investigating the adsorption-desorption behavior of HDTMA-modified zeolite towards diclofenac sodium. The HDTMA-modified zeolite adsorbed the diclofenac sodium of 54.01% at a pH of 7.5, the contact time of 60 min, and the initial concentration of 100 ppm. The adsorbed diclofenac sodium of 73.95% could be released from the HDTMA-modified adsorbent for 8 h, mimicking the time length of drug metabolism in the human body.

2021 ◽  
Vol 18 ◽  
Author(s):  
Subheet Kumar Jain ◽  
Neha Panchal ◽  
Amrinder Singh ◽  
Shubham Thakur ◽  
Navid Reza Shahtaghi ◽  
...  

Background: Diclofenac sodium (DS) injection is widely used in the management of acute or chronic pain and inflammatory diseases. It incorporates 20 % w/v Transcutol-P as a solubilizer to make the stable injectable formulation. However, the use of Transcutol-P in high concentration leads to adverse effects such as severe nephrotoxicity, etc. Some advancements resulted in the formulation of an aqueous based injectable but that too used benzyl alcohol reported to be toxic for human use. Objective: To develop an injectable self-micro emulsifying drug delivery system (SMEDDS) as a novel carrier of DS for prompt release with better safety and efficacy. Methods: A solubility study was performed with different surfactants and co-surfactants. The conventional stirring method was employed for the formulation of SMEDDS. Detailed in vitro characterization was done for different quality control parameters. In vivo studies were performed using Wistar rats for pharmacokinetic evaluation, toxicological analysis, and analgesic activity. Results: The optimized formulation exhibited good physical stability, ideal globule size (156±0.4 nm), quick release, better therapeutics, and safety, increase in LD50 (221.9 mg/kg) to that of the commercial counterpart (109.9 mg/kg). Further, pre-treatment with optimized formulation reduced the carrageenan-induced rat paw oedema by 88±1.2 % after 4 h, compared to 77±1.6 % inhibition with commercial DS formulation. Moreover, optimized formulation significantly (p<0.05) inhibited the pain sensation in the acetic-acid induced writhing test in mice compared to its commercial equivalent with a better pharmacokinetic profile. Conclusion: The above findings confirmed that liquid SMEDDS could be a successful carrier for the safe and effective delivery of DS


2018 ◽  
Vol 7 (4) ◽  
pp. 291-301 ◽  
Author(s):  
Zepeng Jiao ◽  
Bin Zhang ◽  
Chunya Li ◽  
Weicong Kuang ◽  
Jingxian Zhang ◽  
...  

Abstract A drug delivery system based on carboxymethyl cellulose-grafted graphene oxide loaded by methotrexate (MTX/CMC-GO) with pH-sensitive and controlled drug-release properties was developed in this work. CMC was grafted on graphene oxide by ethylenediamine through hydrothermal treatment. CMC serves as a pH-sensitive trigger, while CMC-GO serves as a drug-carrying vehicle due to the curved layer and large plain surface. Different amounts of drugs could be loaded into CMC-GO nanocarriers by control of the original amount of drug/carrier ratios. Additionally, low cytotoxicity against NIH-3T3 cells and low in vivo toxicity was observed. In vivo tumor growth inhibition assays showed that MTX/CMC-GO demonstrated superior antitumor activity than free MTX against HT-29 cells. Moreover, prolonged survival time of mice was observed after MTX/CMC-GO administration. The MTX/CMC-GO drug delivery system has a great potential in colon cancer therapy.


2021 ◽  
Vol 21 (2) ◽  
pp. 824-832
Author(s):  
Zhenzhen Fan ◽  
Qingsheng Liu ◽  
Fangfang Lu ◽  
Zhihui Dong ◽  
Peng Gao

Liver cancer has a high incidence and a poor prognosis, which seriously affects human health. Doxorubicin is one of the chemotherapeutics used in the treatment of tumours, but its severe adverse reactions, especially cardiac toxicity, have limited its clinical application. The nanometre drug delivery system enables drug-loaded nanoparticles to be specifically concentrated in tumour tissues, increasing cell uptake and improving curative effect. Therefore, in this paper, folic acid-modified mesoporous silica nanoparticles (MSN-NH2-PEG-FA) were synthesized by modifying the folic acid on the surface of a drug carrier by using the characteristics of the expression of folic acid receptors, and using it as a drug. The carrier was loaded with antitumor drug doxorubicin hydrochloride (DOX), and a nanometre drug delivery system (MSN-NH2-PEG-FA/DOX) was constructed. At the same time, the near-infrared dye Cy5 was used to mark the mother nucleus to construct fluorescent nanoparticles (MSN-NH2-PEG-FA/DOX-Cy5) for cell and tumour imaging, so as to obtain the abdominal image of liver cancer patients, thereby realizing diagnosis and treatment. The research results show that the carrier can specifically gather in the liver area, reduce the distribution in the heart, reduce the toxic and side effects of drugs, and prolong the survival time of patients. The results of this study provide new ideas for the treatment of liver cancer, and provide a new theoretical basis and experimental basis for the study of inorganic nanomaterials as targeted drug delivery systems.


2005 ◽  
Vol 288-289 ◽  
pp. 125-128 ◽  
Author(s):  
Shen Guo Wang ◽  
Qing Cai ◽  
Jian Zhong Bei ◽  
Wei Yun Shi ◽  
Li Xin Xie

In the article a kind biodegradable drug carrier (glycolide-co-lactide-co-caprolactone) tricomponent copolymer (PGLC) was synthesized by ring opening copolymerization of glycolide (GA), lactide (LA) and ε-caprolactone (CL), and was used to manufacture an implantable drug preparation---Cyclosporine-PGLC drug delivery system (Cs-PGLC DDS).The Cs could slowly release from the Cs-PGLC DDS near linearly and last for a long time in vitro. A clinically significant Cs concentration in the cornea and anterior chamber could be achieved by implanting the Cs-PGLC DDS in anterior chamber. It was demonstrated that the Cs-PGLC DDS is a long-effective intraocular immunosuppressive agent for remaining corneal allograft clear and significantly prolong its survival time.


2015 ◽  
Vol 112 (10) ◽  
pp. 2978-2983 ◽  
Author(s):  
Tuo Wei ◽  
Chao Chen ◽  
Juan Liu ◽  
Cheng Liu ◽  
Paola Posocco ◽  
...  

Drug resistance and toxicity constitute challenging hurdles for cancer therapy. The application of nanotechnology for anticancer drug delivery is expected to address these issues and bring new hope for cancer treatment. In this context, we established an original nanomicellar drug delivery system based on an amphiphilic dendrimer (AmDM), which could generate supramolecular micelles to effectively encapsulate the anticancer drug doxorubicin (DOX) with high drug-loading capacity (>40%), thanks to the unique dendritic structure creating large void space for drug accommodation. The resulting AmDM/DOX nanomicelles were able to enhance drug potency and combat doxorubicin resistance in breast cancer models by significantly enhancing cellular uptake while considerably decreasing efflux of the drug. In addition, the AmDM/DOX nanoparticles abolished significantly the toxicity related to the free drug. Collectively, our studies demonstrate that the drug delivery system based on nanomicelles formed with the self-assembling amphiphilic dendrimer constitutes a promising and effective drug carrier in cancer therapy.


Author(s):  
Ashish B. Budhrani ◽  
Shubhra R. Rai ◽  
Aarati S. Panchbhai ◽  
Rajshri B. Dongarwar

Nano-emulsion dosage forms have nano-sized droplets of disperse phase and are kinetically stable dosage form. Nano-emulsions are included under the category of new drug delivery system containing emulsified water in oil/oil in water system having mean globule size ranges from 10 nm to 1000 nm.  In the field of pharmacy, nano-emulsions play an essential role in the delivery of medication through various drug administration routes like parenteral, topical and oral route. Nano-emulsions are nano-sized emulsions which are used under high investigation as a drug carrier for enhancing the delivery of therapeutic agents. Nano-emulsions have enhanced functional properties as compared to standard emulsions. They are nowadays growing work for utilizing nano-sized particles in the research of pharmaceuticals, cosmetics and food products.  Mainly, intrigue has been creating simultaneously with higher emulsification techniques and mechanisms of stabilization. Nano-emulsions are formulated by both methods like high energy emulsification or low energy emulsification methods. Rapid energy emulsification technique includes high shear mixing, high-pressure homogenization or ultrasonication. In contrast, low energy emulsification technique includes the merit of the physicochemical characteristics of the system, which exploits phase transitions to obtained nano-emulsion. This review article is an effort to summarize comparative aspects like introduction, types, advantages, disadvantages, components, factors affecting, methods of preparations, methods of analysis of nano-emulsion and applications of nano-emulsion.


Nanoscale ◽  
2019 ◽  
Vol 11 (24) ◽  
pp. 11709-11718 ◽  
Author(s):  
Zhongbo Xue ◽  
Mengyao Zhu ◽  
Yuze Dong ◽  
Tong Feng ◽  
Zhuozhi Chen ◽  
...  

Graphdiyne and UIO-66-NH2 form a framework structure as a drug carrier and apply to tumor therapy.


2013 ◽  
Vol 320 ◽  
pp. 495-504 ◽  
Author(s):  
Guo Jing Gou ◽  
Li E Dong ◽  
Feng Juan Bao ◽  
Zhi Yu Wang ◽  
Lin Jiao ◽  
...  

This paper reviewed our research progress in respects of th intercalation law of acetylsalicylic acid (ASP) with magnesium aluminate layered double hydroxide (LDH), the drug release mechanism and the tablet preparation effect of LDH-ASP system. We also discussed the propositions about the composite assembly rules, slow-release mechanism, and dosage form processing of the layered double hydroxide drug delivery system. Intercalation way and drug structure should be taken into consideration in assembly LDH-drugs system. The characteristic parameter of the composite LDH-drug reflected finely their loading efficiency and correlated definitely with drug release property. It had been found that the release rate and extent of intercalated drug was closely linked to the retarding status of LDH interlayer, which was dependent on the exchange mole ratio of n(drug) with n[HnPO4(3-n)-]. In addition, the grafting reaction and phase transformation degree of LDH layer was hinged on the acidity of solution. The slow-release function of the LDH-drug system could be improved significantly by compositing with dextran (DET). A sustained-release skeleton tablet was producted with DET-LDH-ASP drug delivery system and hydrophilic gel material HPMC, which could effectively overcome the "first pass effect" and " burst release problem" of LDH-drug oral agents. The slow-release effect of LDH drug delivery system could be ulteriorly improved in systemic circulation environments, attributed to the triple control of HPMC-DET-LDH, DET-LDH-drugs three-level supramolecular assembly and the special circulation in vivo. Key words: Layered double hydroxide, Supramolecular assembly, Release control, Slow controlled release drug delivery system


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