Application of Methylated N-(4-N,N-Dimethylaminocinnamyl) Chitosan for Oral Protein Drug Delivery

2012 ◽  
Vol 506 ◽  
pp. 465-468
Author(s):  
J. Kowapradit ◽  
Theerasak Rojanarata ◽  
Tanasait Ngawhirunpat ◽  
A. Apirakaramwong ◽  
Warayuth Sajomsang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Entrapment Efficiency ◽  
Egg Yolk ◽  
Molar Ratio ◽  
Protein Drug ◽  
Egg Yolk Phosphatidylcholine ◽  
Model Protein ◽  
Protein Drug Delivery ◽  
Low Cytotoxicity

In the present study, methylated N-(4-N,N-dimethylaminocinnamyl) chitosan (TM65CM50CS) was synthesized and investigated for oral protein drug delivery by combining with liposomes entrapped bovine serum albumin (FITC-BSA), a model protein. FITC-BSA liposomes composed of egg yolk phosphatidylcholine and sodium oleate in molar ratio of 10:2 were prepared by thin film hydration method. The TM65CM50CS coated liposomal FITC-BSA was evaluated for transport of protein and its cytotoxicity in Caco-2 cells. Moreover, the in vitro stability of BSA in TM65CM50CS coated liposomes was also examined by the degradation of protein from pancreatin. The mean particle size and zeta-potential of liposomes were 101+0.02 nm and -27.44+2.02 mV, respectively. Initial FITC-BSA (2.5% w/w) to lipid showed the highest percentage entrapment efficiency (50.13%) and FITC-BSA content (8.08 mg/g of lipid). The results of FITC-BSA transport showed that TM65CM50CS coated FITC-BSA liposomes enhanced protein permeability across Caco-2 cell monolayers with low cytotoxicity. In addition, these liposomes could protect the degradation of protein from pancreatin. Our studies demonstrated that TM65CM50CS coated liposomes have the potential to be used as an oral protein drug delivery.

scholarly journals Modulation of Entrapment Efficiency and In Vitro Release Properties of BSA-Loaded Chitosan Microparticles Cross-Linked with Citric Acid as a Potential Protein–Drug Delivery System

Materials ◽  
2020 ◽  
Vol 13 (8) ◽  
pp. 1989 ◽  
Author(s):  
Natalia Sedyakina ◽  
Andrey Kuskov ◽  
Kelly Velonia ◽  
Nataliya Feldman ◽  
Sergey Lutsenko ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Citric Acid ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Cross Linking ◽  
Release Mechanism ◽  
Model Protein ◽  
Cross Linker ◽  
The Cross

Microparticles, aimed for oral protein and peptide drug delivery, were prepared via emulsion cross-linking using citric acid as cross-linker and polyglycerol polyricinoleate as surfactant. A comparative study of the interaction between chitosan and citric acid and its effect on the resulting microparticle properties was performed using different chitosan-to-cross-linker mass ratios and pH-values during fabrication of the microparticles. Non-cross-linked and cross-linked microparticles were studied in terms of size (4–12 μm), zeta potential (−15.7 to 12.8 mV), erosion (39.7–75.6%), a model protein encapsulation efficiency (bovine serum albumin) (6.8–27.6%), and loading capacity (10.4–40%). Fourier transform infrared spectroscopy and X-ray diffraction confirmed the ionic interaction between the protonated amine groups of chitosan and the carboxylate ions of the cross-linking agent. Scanning electron microscopy revealed that the non-cross-linked microparticles had an uneven shape with wrinkled surfaces, while the cross-linked formulations were spherical in shape with smooth surfaces. On the basis of these data, the role of the surfactant and microparticle structure on the release mechanism was proposed. Control of the microparticle shape and release mechanisms is expected to be crucial in developing carriers for the controlled delivery of proteins and peptides.

scholarly journals EUDRAGIT COATED ALGINATE BEADS BEARING OXALIPLATIN LOADED LIPOSOMES: FORMULATION, OPTIMIZATION AND IN VITRO CHARACTERIZATION

2021 ◽  
pp. 170-177
Author(s):  
ANKITA TIWARI ◽  
SANJAY K. JAIN
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
Alginate Beads ◽  
Molar Ratio ◽  
Specific Drug ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Vesicle Size

Objective: The present investigation aimed to develop and characterize Eudragit S-100 coated alginate beads bearing oxaliplatin loaded liposomes for colon-specific drug delivery. Methods: Liposomes were formulated by the thin-film hydration method. The process and formulation variables were optimized by Box-Behnken design (BBD) with the help of Design-Expert® Software. Three independent variables taken were HSPC: Chol molar ratio (X1), hydration time (X2), and sonication time (X3). The response variables selected were entrapment efficiency of oxaliplatin, polydispersity index, and vesicle size. Results: The liposomes possessed an average vesicle size of 110.1±2.8 nm, PDI 0.096±0.3, zeta potential of-6.70±1.4 mV, and entrapment efficiency of 27.65%. The beads were characterized for their size, in vitro drug release, and swelling index. The degree of swelling of the beads was found to be 2.3 fold higher at pH 7.4 than at pH 1.2. The in vitro drug release depicted a sustained drug release in 48 h. Conclusion: The outcomes of the study proposed that the developed system can be effectively used for site-specific drug delivery to the colon via the oral route.

scholarly journals Preparation of agarose-glucan for anti-tumor necrosis factor protein drug delivery

2018 ◽  
Vol 34 (4) ◽  
Author(s):  
Hường Pham
Keyword(s):  
Drug Delivery ◽  
Tumor Necrosis Factor ◽  
Tumor Necrosis ◽  
Liquid Paraffin ◽  
Protein Drug ◽  
Necrosis Factor Alpha ◽  
Tnf Α ◽  
Model Protein ◽  
Protein Drug Delivery ◽  
Necrosis Factor

Our purpose was to develop and characterize a protein drug delivery system in agarose-glucan complex. The complex was produced by sonicating the mixture of agarose-glucan components and a protein in liquid paraffin with Sonics Vibracell Processor adapted from method of Nuo Wang et all 1997 [1]. We used etanercept, an anti-tumor necrosis factor-alpha (TNF-α) as a model protein drug, which was encapsulated successfully into agarose-glucan complex system. This protein can neutralize the TNF-α, a pro-inflammatory cytokines that plays a pivotal role in regulating the inflammatory response in rheumatoid arthritis (RA) and well known as mediator worsening RA pathogenesis. The agarose-glucan complex we made possessed a range of sizes from 30 to 150 nm, dissolving well within a range of pH buffer from 5.2 to 6.2, an average protein encapsulated efficiency up to 70%, and protein release efficiency of 50% after 24 hours. This research is the base for developing nanogel-size targeted drug delivery in RA treatment.

Effect of Edge Activator on Characteristic and in Vitro Skin Permeation of Meloxicam Loaded in Elastic Liposomes

2011 ◽  
Vol 194-196 ◽  
pp. 537-540 ◽  
Author(s):  
Sureewan Duangjit ◽  
Praneet Opanasopit ◽  
Theerasak Rojanarata ◽  
Tanasait Ngawhirunpat
Keyword(s):  
Drug Delivery ◽  
Transdermal Drug Delivery ◽  
Skin Permeation ◽  
Cetylpyridinium Chloride ◽  
Entrapment Efficiency ◽  
Molar Ratio ◽  
Transdermal Drug Delivery System ◽  
Scanning Calorimetry ◽  
In Vitro Skin Permeation

The aim of this study was to prepare and investigate the potential use of liposomes in the transdermal drug delivery of meloxicam (MX). The vesicles containing a constant amount of MX, phosphatidylcholine (PC), cholesterol (Chol) and cetylpyridinium chloride (CPC) (1:5:1:1 MX/PC/Chol/CPC molar ratio) to obtain liposomes. MX loaded liposomes were investigated for particle size, zeta potential, entrapment efficiency (%EE) and in vitro skin permeation. The results indicated that the liposomes were spherical in structure, 77 to 100 nm in size and charged. The %EE of MX in the vesicles ranged from 55 to 56%. The elastic liposomes consisting of MX/PC/Chol/CPC provided a significantly higher skin permeation of MX compared to the other formulations. Fourier Transform Infrared Spectroscopy (FT-IR) and Differential Scanning Calorimetry (DSC) analysis indicated that the application of liposomes may disrupt the stratum corneum lipid. Our research suggests that MX loaded elastic liposomes can be potentially used as a transdermal drug delivery system.

SUSTAINED RELEASE OF INSULIN FROM POLOXAMER GELS INTERPENETRATED BY POLYION COMPLEXATION OF CHITOSAN-HYALURONIC ACID NETWORK

2010 ◽  
Vol 22 (06) ◽  
pp. 475-480
Author(s):  
Ming-Chia Yang ◽  
Jiun-Sheng Yang ◽  
Yi-You Huang ◽  
Ming-Jium Shieh ◽  
Tze-Wen Chung
Keyword(s):  
Drug Delivery ◽  
Hyaluronic Acid ◽  
Sustained Release ◽  
Insulin Release ◽  
Burst Release ◽  
Protein Drug ◽  
Initial Burst ◽  
Initial Burst Release ◽  
Protein Drug Delivery

This study investigates in vitro the protein drug delivery characteristics of new thermal sensitive gels, poloxamer (P)–chitosan (CS)/hyaluronic acid (HA) gels (P–CS/HA), in which a CS solution is interacting with various concentrations of HA that interpenetrates P gels. The polyion complexation occurs between CS and HA that can protect drugs from proteolysis. The results indicate that the swelling ratios of all P–CS/HA gels are markedly superior to those of nonswelling P and P–CS gels. For example, P–CS/HA (0.5% (w/w)) gels have swelling ratios of 48.3 ± 2.7% (w/w), which are maintained for approximately 0.5 h in water at 37°C. In vitro releases of insulin from P–CS/HA (0.5% (w/w)) gels had significantly lowered initial burst release (P < 0.01) and lasted much longer than those from gels without a CS network. The duration of insulin release was in a significantly sustained manner for up to 3.5 h, which was about two times or longer than the period of delivery using P or P–CS gels.

Development and Characterization Colchicine-Loaded PEGylated Gelatin Nanoparticles for Targeted Delivery to Tumor

2013 ◽  
Vol 6 (2) ◽  
pp. 2058-2063
Author(s):  
G D Chandrethiya ◽  
P K Shelat ◽  
M N Zaveri
Keyword(s):  
Drug Delivery ◽  
Targeted Delivery ◽  
High Performance ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Spherical Particles ◽  
Precipitation Method ◽  
Antitumoral Activity ◽  
Gelatin Nanoparticles

PEGylated gelatin nanoparticles loaded with colchicine were prepared by ethanol precipitation method. Poly-(ethylene glycol)-5000-monomethylether (MPEG 5000), a hydrophilic polymer, was used to pegylate gelatin.  Gluteraldehyde was used as cross-linking agent. To obtain a high quality product, major formulation parameters were optimized.  Spherical particles with mean particles of 193 nm were measured by a Malvern particle size analyzer. Entrapment efficiency was found to be 71.7 ± 1.4% and determined with reverse phase high performance liquid charomatography (RP-HPLC). The in vitro drug release study was performed by dialysis bag method for a period of 168 hours. Lyophilizaton study showed sucrose at lower concentrations proved the best cryoprotectant for this formulation.  Stability study revealed that lyophilized nanoparticles were equally effective (p < 0.05) after one year of storage at 2-8°C with ambient humidity. In vitro antitumoral activity was accessed using the MCF-7 cell line by MTT assay.  The IC50 value was found to be 0.034 μg/ml for the prepared formulation. The results indicate that PEGylated gelatin nanoparticles could be utilized as a potential drug delivery for targeted drug delivery of tumors.  

A Novel Oral Protein-Drug Delivery System with Bilayer Shell-Core Structure

2020 ◽  
Author(s):  
Xuan Zhang ◽  
Yanjun Tong ◽  
Xiaomei Lyu ◽  
Jianfen Ye ◽  
Ruijin Yang
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Core Structure ◽  
Protein Drug ◽  
Protein Drug Delivery

scholarly journals FORMULATION AND EVALUATION OF PERINDOPRIL MICROENCAPSULES BY USING DIFFERENT POLYMER

2017 ◽  
Vol 10 (2) ◽  
pp. 153
Author(s):  
Leena Jacob ◽  
Abhilash Tv ◽  
Shajan Abraham
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Release Rate ◽  
Oral Drug Delivery ◽  
Entrapment Efficiency ◽  
Water Soluble ◽  
Oral Drug ◽  
Percentage Yield ◽  
Drug Entrapment Efficiency

Objective: The study was carried out with an objective to achieve a potential sustained release oral drug delivery system of an antihypertensive drug, Perindopril which is a ACE inhibitor having half life of 2 hours. Perindopril is water soluble drug, so we can control or delay the release rate of drug by using release retarding polymers. This may also decrease the toxic side effects by preventing the high initial concentration in the blood.Method: Microcapsules were prepared by solvent evaporation technique using Eudragit L100 and Ethyl cellulose as a retarding agent to control the release rate and magnesium stearate as an inert dispersing carrier to decrease the interfacial tension between lipophilic and hydrophilic phase. Results: Prepared microcapsules were evaluated for the particle size, percentage yield, drug entrapment efficiency, flow property and in vitro drug release for 12 h. Results indicated that the percentage yield, mean particle size, drug entrapment efficiency and the micrometric properties of the microcapsules was influenced by various drug: polymer ratio. The release rate of microcapsules could be controlled as desired by adjusting the combination ratio of dispersing agents to retarding agents.Conclusion:Perindopril microcapsules can be successfully designed to develop sustained drug delivery, that reduces the dosing frequency and their by one can increase the patient compliance.

scholarly journals NANO-VESICLES OF SALBUTAMOL SULPHATE IN METERED DOSE INHALERS: FORMULATION, CHARACTERIZATION AND IN VITRO EVALUATION

2017 ◽  
Vol 9 (6) ◽  
pp. 100 ◽  
Author(s):  
Mona G. Arafa ◽  
Bassam M. Ayoub
Keyword(s):  
In Vitro Release ◽  
Pulmonary Delivery ◽  
Entrapment Efficiency ◽  
Reversed Phase ◽  
Molar Ratio ◽  
Metered Dose Inhalers ◽  
Salbutamol Sulphate ◽  
Novel Approach ◽  
Metered Dose

Objective: The present work was aimed to prepare niosomes entrapping salbutamol sulphate (SS) using reversed phase evaporation method (REV).Methods: Niosomes were prepared by mixing span 60 and cholesterol in 1:1 molar ratio in chloroform, SS in water was then added to organic phase to form niosomal SS. Formulations after evaporation of chloroform, freeze centrifuged then lyophilized, were evaluated for particles size, polydispersity index (Pdi), zeta-potential, morphology, entrapment efficiency (EE%) and in vitro release. For pulmonary delivery; metered dose inhalers (MDI) were prepared by suspending SS niosomes equivalent to 20 mg SS in hydrofluoroalkane (HFA). The metered valve was investigated for leakage rate, the total number of puffs/canister, weight/puff, dose uniformity and particle size.Results: The results showed spherical niosomes with 400-451 nm particles that entrapped 66.19% of SS. 76.54±0.132% SS release from niosomes that showed a controlled release profile for 8h. The leakage test was not exceeding 4 mg/3 d, the number of puffs were up to 200puffs/canister, the dose delivered/puff was 0.1 mg and 0.64-4.51μm niosomal aerosol.Conclusion: The results indicate an encouraging strategy to formulate a controlled drug delivery by entrapping (SS) in niosomes which could be packaged into (MDI) that met the requirements of (USP) aerosols guidelines which offering a novel approach to respiratory delivery.

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