Synthesis and Performance of pH-Sensitive Hydrogel Microspheres and In Vitro Evaluation as Potential Drug Carriers

2014 ◽  
Vol 936 ◽  
pp. 751-756 ◽  
Author(s):  
Yuan Yuan Liang ◽  
Tong Chen ◽  
Yu Qin Cui ◽  
Rui Qiong Tian ◽  
Tong Sheng Qi ◽  
...  
Keyword(s):  
Drug Carriers ◽  
Gastric Fluid ◽  
Ph Sensitive ◽  
Simulated Gastric Fluid ◽  
Surface Areas ◽  
Ph Responsibility ◽  
Model Drug ◽  
Hydrogel Microspheres ◽  
Ph Sensitive Hydrogel

To accelerate the response rate of smart hydrogels to the environmental conditions, a novel pH-sensitive hydrogel microsphere with the controlled shapes and sizes were developed. Such monodispersed microspheres were synthesizedviafree radical polymerization under the protection of a multilayer stability system. The pH-responsibility of hydrogel microspheres was tested with the hydrogel bulk as a control.In vitrorelease studies were conducted in the simulated gastric fluid and intestinal juice with bovine serum albumin (BSA) as a model drug. The large specific surface areas endowed hydrogel microspheres a faster pH-responsibility than that of bulk ones. Therefore, such microspheres showed potential applications as the oral protein drugs carrier.

Synthesis and performance of pH-sensitive hydrogel microspheres and in vitro evaluation as potential drug carriers

2014 ◽  
Vol 21 (11) ◽  
pp. 2287-2296 ◽  
Author(s):  
Ruiqiong Tian ◽  
Yuanyuan Liang ◽  
Xiaoyun Zhang ◽  
Yuqin Cui ◽  
Yingge Zhao ◽  
...  
Keyword(s):  
Drug Carriers ◽  
Ph Sensitive ◽  
Potential Drug ◽  
In Vitro Evaluation ◽  
And Performance ◽  
Hydrogel Microspheres ◽  
Ph Sensitive Hydrogel

scholarly journals Formulation of Quaternized Aminated Chitosan Nanoparticles for Efficient Encapsulation and Slow Release of Curcumin

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 449
Author(s):  
Ahmed M. Omer ◽  
Zyta M. Ziora ◽  
Tamer M. Tamer ◽  
Randa E. Khalifa ◽  
Mohamed A. Hassan ◽  
...  
Keyword(s):  
Slow Release ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
Gastric Fluid ◽  
Release Profile ◽  
Simulated Gastric Fluid ◽  
Maximum Value ◽  
Structure Surface ◽  
Drug Encapsulation Efficiency

An effective drug nanocarrier was developed on the basis of a quaternized aminated chitosan (Q-AmCs) derivative for the efficient encapsulation and slow release of the curcumin (Cur)-drug. A simple ionic gelation method was conducted to formulate Q-AmCs nanoparticles (NPs), using different ratios of sodium tripolyphosphate (TPP) as an ionic crosslinker. Various characterization tools were employed to investigate the structure, surface morphology, and thermal properties of the formulated nanoparticles. The formulated Q-AmCs NPs displayed a smaller particle size of 162 ± 9.10 nm, and higher surface positive charges, with a maximum potential of +48.3 mV, compared to native aminated chitosan (AmCs) NPs (231 ± 7.14 nm, +32.8 mV). The Cur-drug encapsulation efficiency was greatly improved and reached a maximum value of 94.4 ± 0.91%, compared to 75.0 ± 1.13% for AmCs NPs. Moreover, the in vitro Cur-release profile was investigated under the conditions of simulated gastric fluid [SGF; pH 1.2] and simulated colon fluid [SCF; pH 7.4]. For Q-AmCs NPs, the Cur-release rate was meaningfully decreased, and recorded a cumulative release value of 54.0% at pH 7.4, compared to 73.0% for AmCs NPs. The formulated nanoparticles exhibited acceptable biocompatibility and biodegradability. These findings emphasize that Q-AmCs NPs have an outstanding potential for the delivery and slow release of anticancer drugs.

scholarly journals Semi-Crystalline Copolymer Hydrogels as Smart Drug Carriers: In Vitro Thermo-Responsive Naproxen Release Study

Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 158
Author(s):  
Snežana Ilić-Stojanović ◽  
Ljubiša Nikolić ◽  
Vesna Nikolić ◽  
Slobodan Petrović ◽  
Violeta Oro ◽  
...  
Keyword(s):  
Drug Carrier ◽  
Drug Carriers ◽  
Xrd Analysis ◽  
Hplc Method ◽  
Potential Candidate ◽  
Swelling Kinetic ◽  
Model Drug ◽  
Xrd Techniques ◽  
Responsive Hydrogels

In this study, poly(N-isopropylacrylamide-co-2-hydroxypropyl methacrylate) hydrogels were synthesized using free radical initiated copolymerization method. Four hydrogels with different cross-linker concentrations were prepared. Semi-crystalline, cross-linked copolymer networks were confirmed by FTIR, SEM and XRD analysis. Variation of swelling behaviour was monitored gravimetrically and thermo-responsiveness has been noticed. An application of synthesized thermo-responsive hydrogels as carriers for the modulated release of anti-inflammatory model drug was investigated. Moreover, naproxen loading into these hydrogels was also determined using FTIR, SEM and XRD techniques and release was analyzed using HPLC method at simulated physiological conditions. Swelling kinetic and mechanism of water transport, as well as diffusion of naproxen through the hydrogels were analyzed. Thus, the aim of this work was to study various compositions of obtained hydrogels and their possibility of application as a thermo-responsive carrier for prolonged naproxen release in order to evaluate as a potential candidate for drug carrier in future pharmaceutical applications.

scholarly journals Safety Assessment of Nano-Hydroxyapatite as an Oral Care Ingredient according to the EU Cosmetics Regulation

Cosmetics ◽  
2018 ◽  
Vol 5 (3) ◽  
pp. 53 ◽  
Author(s):  
Joana Ramis ◽  
Catarina Coelho ◽  
Alba Córdoba ◽  
Paulo Quadros ◽  
Marta Monjo
Keyword(s):  
Oral Care ◽  
Gastric Fluid ◽  
Gingival Tissue ◽  
Simulated Gastric Fluid ◽  
Tem Analysis ◽  
Consumer Safety ◽  
Transmission Electron ◽  
Dissolution Behaviour ◽  
Gingival Epithelium

Hydroxyapatite nanoparticles (HAP-NP) are incorporated in oral care products such as toothpastes and mouthwashes to treat dental sensitivity or to promote enamel remineralisation. Despite the good performance of HAP-NP in this application, it is important to ensure its safety for consumers. For that reason, the Scientific Committee on Consumer Safety (SCCS) evaluated the safety of HAP-NP as an oral care ingredient, but the issued opinion was not completely conclusive and the SCCS recommended that additional tests should be performed. Here, we used a commercially available human gingival epithelium (HGE) as a non-animal alternative and MTT cell viability, LDH activity, and IL-1alpha production were evaluated after 3.1% HAP-NP treatment for 10 min, 1 h, and 3 h. Moreover, the absorption of HAP-NP in the gingival tissue was assessed by transmission electron microscopy (TEM) analysis. Finally, the dissolution behaviour of HAP-NP in simulated gastric fluid was also investigated. No deleterious effect was observed for HGE tissues incubated with HAP-NP for all time-points and parameters evaluated. Moreover, a complete dissolution of 3.1% HAP-NP in simulated gastric fluid was observed after 7.5 min at 37 °C. In conclusion, our results evidence the safety of HAP-NP for oral care products with the use of an in vitro replacement alternative for human gingival epithelium and a simulated gastric fluid assay.

scholarly journals A Facile Route to Fabricate CS/GO Composite Film for the Application of Therapeutic Contact Lenses

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Pin Chen ◽  
Xin Wang ◽  
Jingyang Kong ◽  
Xiaohong Hu
Keyword(s):  
Composite Film ◽  
Contact Lenses ◽  
Umbilical Vein ◽  
Drug Carriers ◽  
Diffusion Method ◽  
Swelling Ratio ◽  
Significant Difference ◽  
Ophthalmic Drug ◽  
Model Drug

Traditional contact lenses bring convenience for ophthalmic drug delivery. However, either as contact lenses or as drug carriers, traditional materials have still some drawbacks in the field. Therefore, a transparent film was designed and investigated for the application of therapeutic contact lenses. Chitosan (CS)/graphene oxide (GO) composite film and CS film were fabricated with acceptable transparent and tensile properties by simple casting flow method. Although swelling ratio of CS/GO composite film was higher than that of CS film with significant difference, both formed films had suitable swelling ratio for contact lens application. Both CS/GO composite film and CS film exhibited typical CS infrared characteristic peaks. CS/GO composite film had significant greater breaking strength than CS film, but its elongation at break was a little lower than CS film. Either CS/GO composite film or CS film exhibited good hydrophilic property with a contact angle of around 20 degree. Ofloxacin as a model drug was loaded into films by adsorption diffusion method. Loaded drug amount in CS/GO composite film was a little larger than that in CS film, but without significant difference. The drug release behaviors from CS/GO composite film or CS film were investigated and revealed that the loaded drug could be controlled to release in the first hour. Two kinds of cells were used to evaluate the biocompatibility of films by in vitro method. It was found that both CS/GO composite film and CS film could support human umbilical vein endothelial cell (HUVEC) growth. But for human epidermal fibroblasts (HSF) cells, CS/GO composite film could promote HSF cells growth and proliferation much better than CS film.

scholarly journals THE USE OF CLINOPTILOLITES AS CARRIER OF METFORMIN HYDROCHLORIDE IN DRUG DELIVERY SYSTEM: IN VITRO DRUG RELEASE STUDY

2018 ◽  
Vol 11 (11) ◽  
pp. 285
Author(s):  
Putra Imwa ◽  
Kusumawati Igaw
Keyword(s):  
Drug Release ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Metformin Hydrochloride ◽  
Simulated Intestinal Fluid ◽  
In Vitro Drug Release ◽  
Encapsulation Process ◽  
N2 Sorption ◽  
Metformin Hcl

Objective: As an antidiabetic drug, metformin hydrochloride (HCl) has been well known to possess low oral bioavailability and short half-life. In this study, we prepared the drug delivery system (DDS) of metformin HCl and clinoptilolite as its carrier. The in vitro drug release profile was further investigated.Methods: DDS was made by encapsulating metformin HCl on clinoptilolite using the wet impregnation method at various pH and initial concentration of metformin HCl. Fourier transform infrared spectrometer (FTIR), X-ray diffractometer (XRD), and N2 Sorption Analyzer were used to characterize the as-synthesized DDS. Drug release study was conducted by stirring the DDS in simulated gastric fluid and simulated intestinal fluid over 12 h.Results: The encapsulation process was achieved optimally at pH 7.0 and initial concentration of metformin HCl of 300 mg/l (CLI2-300 denoted DDS). The results of FTIR and N2 sorption analyzer confirmed the existence of metformin HCl on clinoptilolites. Meanwhile, the XRD result showed that the crystallinity of clinoptilolites remained unchanged after the encapsulation process. The cumulative drug release in the simulated gastric fluid was found to be higher than that in the simulated intestinal fluid, which indicated the potent influence of pH on the release properties of the drugs. The drug release kinetics of metformin HCl from clinoptilolite was best fitted into the Korsmeyer-Peppas model with non-Fickian transport mechanism.Conclusion: We found that clinoptilolite was suitable for DDS application, particularly as a carrier of metformin HCl.

scholarly journals Preparation, Characterization, and In Vitro Evaluation of Resveratrol-Loaded Cellulose Aerogel

Materials ◽  
2020 ◽  
Vol 13 (7) ◽  
pp. 1624
Author(s):  
Lili Qin ◽  
Xinyu Zhao ◽  
Yiwei He ◽  
Hongqiang Wang ◽  
Hanjing Wei ◽  
...  
Keyword(s):  
High Speed ◽  
Drug Carrier ◽  
Phosphate Buffer Solution ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Oxidized Cellulose ◽  
Buffer Solution ◽  
Aggregation State ◽  
Cellulose Aerogel

Resveratrol is a natural active ingredient found in plants, which is a polyphenolic compound and has a variety of pharmaceutical uses. Resveratrol-loaded TEMPO-oxidized cellulose aerogel (RLTA) was prepared using a freeze-drying method, employing high speed homogenization followed by rapid freezing with liquid nitrogen. RLTAs were designed at varying drug–cellulose aerogel ratios (1:2, 2:3, 3:2, and 2:1). It could be seen via scanning electron microscopy (SEM) that Res integrated into TEMPO-oxidized cellulose (TC) at different ratios, which changed its aggregation state and turned it into a short rod-like structure. Fourier transform infrared (FTIR) spectra confirmed that the RLTAs had the characteristic peaks of TC and Res. In addition, X-ray diffraction (XRD) demonstrated that the grain size of RLTA was obviously smaller than that of pure Res. RLTAs also had excellent stability in both simulated gastric fluid and phosphate buffer solution. The drug release rate was initially completed within 5 h under a loading rate of 30.7 wt%. The results of an MTT assay showed the low toxicity and good biocompatibility of the RLTAs. TC aerogel could be a promising drug carrier that may be widely used in designing and preparing novel biomedicine.

scholarly journals The Antioxidant Properties of Pectin Fractions Isolated from Vegetables Using a Simulated Gastric Fluid

2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Vasily V. Smirnov ◽  
Victoria V. Golovchenko ◽  
Fedor V. Vityazev ◽  
Olga A. Patova ◽  
Nikolay Yu. Selivanov ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Antioxidant Properties ◽  
Sweet Pepper ◽  
Structural Features ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Oxygen Species ◽  
Pectic Polysaccharides ◽  
White Cabbage

The antioxidant properties of vegetable pectin fractions against intraluminal reactive oxygen species were elucidated in vitro in conjunction with their structural features. The pectin fractions were isolated using a simulated gastric fluid (pH 1.5, pepsin 0.5 g/L, 37°C, 4 h) from fresh white cabbage, carrot, onion, and sweet pepper. The fraction from onion was found to inhibit the production of superoxide radicals by inhibiting the xanthine oxidase. The high molecular weight of onion pectin and a large number of galactose residues in its side chains appeared to participate in interaction with xanthine oxidase. All the isolated pectic polysaccharides were found to be associated with protein (2–9%) and phenolics (0.5–0.7%) as contaminants; these contaminants were shown to be responsible for the antioxidant effect of vegetable pectin fractions against the hydroxyl and 1,1-diphenyl-2-picrylhydrazyl radicals.

Enzyme-Resistant Starch for Oral Colon-Targeting Drug Delivery System

2005 ◽  
Vol 288-289 ◽  
pp. 129-132 ◽  
Author(s):  
Ling Chen ◽  
Xiao Xi Li ◽  
Lin Li ◽  
Bing Li
Keyword(s):  
Drug Delivery ◽  
Resistant Starch ◽  
Drug Carriers ◽  
Enzymatic Digestion ◽  
Oral Route ◽  
X Ray Diffraction ◽  
Colon Targeting ◽  
Potential System ◽  
Model Drug

Colon-targeting drug delivery systems (CDDSs) are employed to improve the bioavailability of protein and peptide drugs through the oral route. So it is important to prepare the drug carriers for oral CDDS. In this study, the Enzyme-Resistant starch (RS) was studied for use as a vehicle in oral colon-targeting drug delivery. The characteristics of RS powders were investigated by X-ray diffraction, polarizing microscopy, DSC and SEM, and their film were examined by enzymatic digestion test. The results showed that RS could be a promising film-former for pharmaceutical coatings, having good stability to enzymatic digestion. Furthermore, a novel peroral formulation using RS coating and bovine serum albumin as a model drug was studied for colon-specific drug delivery in vitro. Drug release studies have shown that RS coating could delivery the drug to the colon and the release rate in simulated colonic fluids was dependent on the biodegradation of RS and its coatings. It is indicated that the RS coated tablet is a potential system for oral CDDS.

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