scholarly journals Fabrication of Quaternized Chitosan Nanoparticles Using Tripolyphosphate/Genipin Dual Cross-Linkers as a Protein Delivery System

Polymers ◽  
2018 ◽  
Vol 10 (11) ◽  
pp. 1226 ◽  
Author(s):  
Kuo-Yu Chen ◽  
Si-Ying Zeng
Keyword(s):  
Protein Delivery ◽  
Drug Carrier ◽  
Chitosan Nanoparticles ◽  
Weight Ratio ◽  
Water Soluble ◽  
Trimethylammonium Chloride ◽  
Sustained Delivery ◽  
Release Studies ◽  
Predicted Values

Various amounts of 2-((acryloyloxy)ethyl)trimethylammonium chloride were grafted onto chitosan (CS) via redox polymerization method to obtain water-soluble quaternized CS (QCS). The QCS nanoparticles loaded with bovine serum albumin (BSA) were then produced by ionic gelation with tripolyphosphate (TPP) and further covalently cross-linked with genipin. The formation of QCS nanoparticles was optimized as a function of monomer grafting yield, QCS/TPP weight ratio, and QCS/genipin weight ratio by Box-Behnken design and response surface methodology. The results showed that QCS nanoparticles prepared with a grafting yield of 50%, QCS/TPP weight ratio of 7.67, and QCS/genipin weight ratio of 60 had a particle size of 193.68 ± 44.92 nm, polydispersity of 0.232, zeta potential of +23.97 mV and BSA encapsulation efficiency of 46.37 ± 2.89%, which were close to the predicted values from mathematical models. In vitro drug release studies at pH 1.2 and pH 7.4 exhibited that the release rate of BSA was significantly decreased and the release period was significantly prolonged after QCS nanoparticles cross-linking with genipin. Therefore, QCS nanoparticles cross-linked with TPP/genipin dual cross-linkers may be a promising protein drug carrier for a prolonged and sustained delivery.

scholarly journals Electrospinning Preparation of Timosaponin B-II-Loaded PLLA Nanofibers and Their Antitumor Recurrence Activities In Vivo

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Zhonghua Huo ◽  
Yan Qiu ◽  
Zhuling Chu ◽  
Peng Yin ◽  
Wenquan Lu ◽  
...  
Keyword(s):  
Drug Carrier ◽  
Amorphous State ◽  
Water Soluble ◽  
Sustained Delivery ◽  
Water Soluble Drug ◽  
Release Studies ◽  
Long Time ◽  
Model Drug

Poly(L-lactic)-acid (PLLA) as a drug carrier and a water-soluble drug timosaponin B-II (TB-II) as a model drug were selected to prepare drug-loaded nanofibers by electrospinning. The average diameters of pure PLLA nanofibers and TB-II-loaded nanofibers were 212.5 ± 68.5, 219.7 ± 57.8, 232.8 ± 66.9, and 232.9 ± 97.7 nm, respectively. DSC and XRD results demonstrated that TB-II was well incorporated into the nanofibers in an amorphous state. FI-TR spectroscopy indicated that TB-II had good compatibility with PLLA. In vitro release studies showed that TB-II was rapidly released from the nanofibers within 6 h, followed by a gradual release for long time. In vivo biosafety test revealed no noticeable toxicity of these TB-II nanofibers. The TB-II released from the nanofibers had obvious inhibition effect against human hepatocellular carcinoma SMMC 7721 cells both in vivo and in vitro. It was confirmed that the TB-II-loaded nanofibers were a sustained delivery system which could effectively inhibit the tumor growth and recurrence after surgery.

scholarly journals DEVELOPMENT AND IN VITRO DISSOLUTION STUDY OF BINARY AND TERNARY SOLID DISPERSIONS OF ACECLOFENAC

2019 ◽  
Author(s):  
Md. Shahidul Islam ◽  
Rasheda Akter Lucky
Keyword(s):  
Polyethylene Glycol ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Weight Ratio ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Peg 6000

The poor aqueous solubility of the drug exhibits in variable dissolution rate and hence poor bioavailability. Aceclofenac is poorly water soluble drug. The aim of the present study was to improve the water solubility and the dissolution rate of Aceclofenac by solid dispersion technique using different water soluble polymers. The term solid dispersions refer to the dispersions of one or more active ingredients in an inert carrier or matrix at solid state. In this study, binary solid dispersion of Aceclofenac were prepared by fusion method using Polyethylene glycol 6000 (PEG 6000), Polyethylene glycol 4000 (PEG 4000), Poloxamer as carrier. Different drug-carrier weight ratio was used for this study. The effect of the carrier on the solubility and in-vitro dissolution were studied. It was found the drug was released 26.86% after 5 minutes and only 40.19% within 60 mins from active Aceclofenac on the other hand the release pattern of Aceclofenac from the binary SD formulation containing PEG 6000 in 1:5 ratio (Formulation coding: A5) showed the best result in comparison of other binary and ternary SD formulations which was 62.29% after 5 min and 83.03% within 60 mins. The hydrophilic polymers used for the preparation of solid dispersion are showed significant increase in the solubility of Aceclofenac.

Preparation of Chitosan Nanoparticles for Protein Delivery by w/o/w Emulsion Solvent Evaporation and Simple Ionotropic Gelation Techniques

2007 ◽  
Vol 121-123 ◽  
pp. 751-754 ◽  
Author(s):  
Garnpimol C. Ritthidej ◽  
W. Pichayakorn ◽  
Chulalongkorn Kusonwiriyawong ◽  
V. Lipipun
Keyword(s):  
Protein Delivery ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Form Complex ◽  
Ionotropic Gelation

The purpose of this study was to prepare chitosan nanoparticles (CS NP) for controlled protein delivery. Two techniques, simple ionotropic gelation (method [I]) and w/o/w emulsion solvent evaporation containing ionotropic gelation (method [II]), were used to prepare CS NP. Tripolyphosphate (TPP) and Eudragit L100-55 (Eud) were used as anionic agents to form complex with cationic chitosan. Bovine serum albumin (BSA) was encapsulated into NP. The morphological characteristics, particle size and size distribution, protein entrapment efficiency, zeta potential, in vitro release, protein secondary structure and its integrity were investigated. The results showed that CS NP could be prepared by appropriate cationic and anionic ratios in both methods. Excess anionic agents resulted in particle aggregation of micron size. The median sizes of particles were between 0.127-0.273 mcm with method [I] provided the smallest size. The 0.02-0.10% BSA loaded preparations showed the same particle sizes and size distributions as blank preparations. SEM photomicrographs revealed that the obtained NP were spherical. Protein entrapment efficiency was between 47-84% and increased when decreasing the percentage of drug loading. The method [II] with TPP exhibited the highest protein entrapment efficiency, following by the method [II] with Eud and method [I] with TPP, respectively. The zeta potentials were positive. Prolonged in vitro protein release profiles were observed from all preparations of CS NP. After 10 days, the release was between 53-72%. Circular dichroism and SDS-polyaceylamide gel electrophoresis techniques confirmed that these processes did not have any destructive effect on the protein structure. Therefore these preparation techniques could be used to encapsulate water-soluble drugs, proteins, DNA, or antigens into CS NP as effective delivery carriers.

scholarly journals Preparation and Characterization of Water-Soluble Chitosan Nanoparticles as Protein Delivery System

2010 ◽  
Vol 2010 ◽  
pp. 1-5 ◽  
Author(s):  
Hong-liang Zhang ◽  
Si-hui Wu ◽  
Yi Tao ◽  
Lin-quan Zang ◽  
Zheng-quan Su
Keyword(s):  
Delivery System ◽  
Protein Delivery ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
Water Soluble ◽  
Preparation Conditions ◽  
Model Drug ◽  
Size And Morphology

The objective of this study was to investigate the potential of water soluble chitosan as a carrier in the preparation of protein-loaded nanoparticles. Nanoparticles were prepared by ionotropic gelation of water-soluble chitosan (WSC) with sodium tripolyphosphate (TPP). Bovine serum albumin (BSA) was applied as a model drug. The size and morphology of the nanoparticles were investigated as a function of the preparation conditions. The particles were spherical in shape and had a smooth surface. The size range of the nanoparticles was between 100 and 400 nm. Result of the in vitro studies showed that the WSC nanoparticles enhance and prolong the intestinal absorption of BSA. These results also indicated that WSC nanoparticles were a potential protein delivery system.

scholarly journals In Vitro MCF-7 Cells Apoptosis Analysis of Carboplatin Loaded Silk Fibroin Particles

Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1110
Author(s):  
Nanyak Galam ◽  
Pinar Tulay ◽  
Terin Adali
Keyword(s):  
Breast Cancer ◽  
Silk Fibroin ◽  
Drug Carrier ◽  
Release Studies ◽  
Apoptotic Effect ◽  
Student’S T ◽  
Drug Carrier System ◽  
Mcf 7

Breast cancer ranks as the fifth leading cause of death worldwide. Chemotherapy is commonly used directly or as neo-adjuvant therapy for the management of breast cancer with its attendant adverse effects, underscoring the need to develop biocompatible bioactive compounds for pharmacological applications. The aim of this study is to encapsulate carboplatin (CP) with silk fibroin protein (SF) by using an ionic gelation method as a drug carrier system and assess the apoptotic effect on MCF-7 breast cancer cells during in vitro studies. The characterization of silk fibroin encapsulated carboplatin (SFCP) microparticles was analyzed by FTIR spectrophotometer, SEM, Mastersizer, and biodegradation methods. The encapsulation efficiency and release profile of SFCP microparticles were analyzed by an indirect UV–Vis spectrophotometric method. An apoptotic screening of MCF-7 cells was carried out with 10–200 µg/mL CP loaded SFCP, which were cultured for 24, 48, and 72 h. Data were analyzed using the Student’s t test and analysis of variance. FTIR and drug release studies confirmed an interaction of silk fibroin with the carboplatin moiety. SFCP showed successful encapsulation of the carboplatin moiety. Apoptotic screening showed a dose dependent increase in absorbance, indicating significant cell death (p < 0.05). Thus, the direct apoptotic effect of SFCP microparticles on MCF-7 was confirmed.

scholarly journals Different BCS Class II Drug-Gelucire Solid Dispersions Prepared by Spray Congealing: Evaluation of Solid State Properties and In Vitro Performances

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 548 ◽  
Author(s):  
Serena Bertoni ◽  
Beatrice Albertini ◽  
Nadia Passerini
Keyword(s):  
Solid State ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Class Ii ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Crystalline Solid ◽  
Dissolution Behavior ◽  
Bcs Class Ii

Delivery of poorly water soluble active pharmaceutical ingredients (APIs) by semi-crystalline solid dispersions prepared by spray congealing in form of microparticles (MPs) is an emerging method to increase their oral bioavailability. In this study, solid dispersions based on hydrophilic Gelucires® (Gelucire® 50/13 and Gelucire® 48/16 in different ratio) of three BCS class II model compounds (carbamazepine, CBZ, tolbutamide, TBM, and cinnarizine, CIN) having different physicochemical properties (logP, pKa, Tm) were produced by spray congealing process. The obtained MPs were investigated in terms of morphology, particles size, drug content, solid state properties, drug-carrier interactions, solubility, and dissolution performances. The solid-state characterization showed that the properties of the incorporated drug had a profound influence on the structure of the obtained solid dispersion: CBZ recrystallized in a different polymorphic form, TBM crystallinity was significantly reduced as a result of specific interactions with the carrier, while smaller crystals were observed in case of CIN. The in vitro tests suggested that the drug solubility was mainly influenced by carrier composition, while the drug dissolution behavior was affected by the API solid state in the MPs after the spray congealing process. Among the tested APIs, TBM-Gelucire dispersions showed the highest enhancement in drug dissolution as a result of the reduced drug crystallinity.

scholarly journals Development and Characterization of Glimepiride Novel Solid Nanodispersion for Improving Its Oral Bioavailability

2020 ◽  
Vol 88 (4) ◽  
pp. 52
Author(s):  
Mona Qushawy ◽  
Ali Nasr ◽  
Shady Swidan ◽  
Yasmin Mortagi
Keyword(s):  
Solid Dispersion ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Water Soluble ◽  
Production Yield ◽  
Scanning Calorimetry ◽  
Differential Scanning Calorimetry Study ◽  
Drug Content ◽  
Vitro Release

Glimepiride is an antidiabetic drug which is one of the third generation sulfonylureas. It belongs to class II, according to the BCS (Biopharmaceutical Classification System), which is characterized by low solubility and high permeability. The aim of this work was to formulate glimepiride as solid dispersion using water-soluble carriers to enhance its aqueous solubility and thus enhance its bioavailability. Nine formulations of glimepiride solid dispersion were prepared by a solvent evaporation technique using three different carriers (mannitol, polyethylene glycol 6000, and β-cyclodextrin) with three different drug carrier ratio (1:1, 1:3, and 1:6). Formulation variables were optimized using 32 full factorial design. The prepared formulations were evaluated for production yield, drug content, micromeritic properties, thermal analysis, in-vitro release, and in-vivo hypoglycemic effect. All prepared formulations showed high production yield ranged from 98.4 ± 2.8 to 99.8 ± 2.2% and high drug content in the range of 97.2 ± 3.2 to 99.6 ± 2.1%. The micromeritic properties revealed that all prepared glimepiride formulations showed good flowability. The differential scanning calorimetry study revealed the presence of the drug in the more soluble amorphous form. In accordance with the results of in vitro release study, it was found that the solubility of glimepiride was increased by increasing the drug carrier ratio, compared with the pure form of the drug. It was found that F9 showed a high and rapid reduction in blood glucose levels in diabetic rats, which indicated the success of a solid dispersion technique in improving the solubility and hence the bioavailability of glimepiride.

Study on the Lipid-Lowering Effect of Water-Soluble Chitosan Nanoparticles and Microspheres In Vitro

2011 ◽  
Vol 217-218 ◽  
pp. 306-310 ◽  
Author(s):  
Bing Gao ◽  
Si Hui Wu ◽  
Hong Liang Zhang ◽  
Yi Tao ◽  
Zheng Quan Su
Keyword(s):  
Binding Capacity ◽  
Food Additives ◽  
Chitosan Nanoparticles ◽  
Water Soluble ◽  
Lipid Lowering ◽  
Drying Methods ◽  
Particle Sizes ◽  
Particle Sizer ◽  
Lipid Lowering Effect

Objective: To prepare water-soluble chitosan(WSC) nanoparticles(WSC-NPs) and microspheres(WSC-MPs) , exam the morphology and particle sizes of them and study their effect on lowering lipids . Methods: WSC-NPs and WSC-MPs were prepared by ionic gelation process and spray-drying methods respectively. The effect of WSC-NPs and WSC-MPs on lowering lipids was evaluated by measuring its binding capacities of lipids in the conditions simulating human gastrointestinal tract in vitro. Also, the morphology and particle sizes of WSC-NPs and WSC-MPs were examined under scanning electron microscopy (SEM) and particle sizer. Resluts: WSC-NPs and WSC-MPs were nearly spherical in shape and the mean particles size varied from 200-400 nm and 3-7 μm respectively; The lipids-binding capacities of WSC-NPs and WSC-MPs were more effective compared with water-soluble chiosan. The lipids-binding capacity were enhenced when the particle size were decreased. Conclusion: WSC-NPs and WSC-MPs will be better fat-lowing food additives to replace water-soluble chitosan.

Fabrication of Degradable Microsphere/PNIPAAm Hydrogel Combination Systems for Protein Delivery

2010 ◽  
Vol 160-162 ◽  
pp. 1072-1076 ◽  
Author(s):  
Ju Yang ◽  
Dan Qun Huo ◽  
Chang Jun Hou ◽  
Guo Ping Zhang ◽  
Li Min Yang ◽  
...  
Keyword(s):  
Protein Delivery ◽  
In Vitro Release ◽  
Great Promise ◽  
Burst Release ◽  
Sustained Delivery ◽  
Plga Microspheres ◽  
Vis Spectroscopy ◽  
Combination System ◽  
Novel Protein

A novel protein delivery system with incorporating PLGA microspheres into porous PNIPAAm hydrogel for sustained delivery of proteins was successfully developed. Distribution of PLGA microspheres in the hydrogel was determined by SEM, and the in vitro protein release characteristics of combination system were investigated by UV-vis spectroscopy. The SEM results showed that PLGA microspheres were encased into the interconnected porous structure of PNIPAAm hydrogel. In vitro release of BSA from combination system exhibited a less burst release followed by a slower sustained release for 20 days. The slow release after the initial burst release was due to the low permeability of BSA in PLGA microspheres. The controlled release of BSA encapsulated within microspheres embedded in scaffolds was better controlled when compared to delivery from PNIPAAm hydrogels alone. The combination systems showed great promise for application in protein delivery.

scholarly journals Anticancer Activity of Water-Soluble Olsalazine-PAMAM-Dendrimer-Salicylic Acid-Conjugates

Biomolecules ◽  
2019 ◽  
Vol 9 (8) ◽  
pp. 360
Author(s):  
Sandra Cortez-Maya ◽  
Luis Daniel Pedro-Hernández ◽  
Elena Martínez-Klimova ◽  
Teresa Ramírez-Ápan ◽  
Marcos Martínez-García
Keyword(s):  
Salicylic Acid ◽  
Anticancer Agents ◽  
Drug Carrier ◽  
Pamam Dendrimer ◽  
Water Soluble ◽  
Mammary Adenocarcinoma ◽  
African Green Monkey Kidney ◽  
Mammary Adenocarcinoma Cell ◽  
Antiproliferative Agent

Improving the activity and selectivity profile of anticancer agents will require designing drug carrier systems that employ soluble macromolecules. Olsalazine-PAMAM-dendrimer-salicylic acid-conjugates with dendritic arms of different lengths have shown good stability regarding the chemical link between drug and spacer. In this study, the drug release was followed in vitro by ultraviolet (UV) studies. Evaluation of the cytotoxicity of the olsalazine-PAMAM-dendrimer-salicylic acid-conjugates employing a sulforhodamine B (SRB) assay in PC-3 (human prostatic adenocarcinoma) and MCF-7 (human mammary adenocarcinoma) cell lines demonstrated that conjugate 9 was more active as an antiproliferative agent than cisplatin, and no cytotoxicity towards the African green monkey kidney fibroblast (COS-7) cell line was observed in any of the conjugates synthesized in the present work.

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