Synthesis, characterization and sustaining controlled release effect of mesoporous SBA-15/ramipril composite drug

A loading of ramipril in SBA-15 (Santa Barbara Amorphous) mesoporous material was studied. (SBA-15)-ramipril composite material was characterized by chemical analysis, infrared spectroscopy, powder X-ray diffraction, low temperature N₂ adsorption–desorption at 77 K characterization techniques. Ramipril drug release processes from SBA-15 host to simulated body fluid (SBF), simulated gastric juice (SGJ), simulated intestinal fluid (SIF) were monitored in a simulated way and actions of the sustained release of (SBA-15)-ramipril was studied. The results showed that the loading amount of ramipril drug in SBA-15 was 90.30 mg/g. The cumulative sustained release rate of ramipril composite drug in SBF achieved 99.7 % after 27 h. When the sustained release of composite drug in SGJ was 8 h, the maximum cumulative sustained release ratio achieved 54.9 %. When the sustained release of composite drug was 9 h in SIF, the maximum cumulative sustained release ratio achieved 34.9 %. The method described in this study is suitable for carrying ramipril drug on SBA-15, and a new carrier to load ramipril drug was found. Meanwhile, the efficacy of ramipril drug and time efficacy could be improved.     

Sodium alginate/HPMC/liquid paraffin emulsified (o/w) gel beads,by factorial design approach; and in vitro analysis

The present study involved development of a novel sodium alginate (SA)/HPMC/light liquid paraffin emulsified (o/w) gel beads containing Diclofenac sodium (DS) as an active pharmaceutical ingredient and its site specific delivery by using hard gelatin capsule fabricated by enteric coated Eudragit L-100 polymer. Emulsified gel beads were formulated by 3-level factorial design, ionic gelatin method. The obtained beads were characterized by Fourier transform infrared, X-ray diffraction and Field emission scanning electron microscope analysis. The variables such as SA (X₁), HPMC (X₂), were optimized for drug loading and in vitro drug release with the help of response surface methodology (RSM). The RSM analysis predicted that SA was significant for both drug loading (p = 0.0005) and drug release (p = 0.0041). HPMC was only significant for drug release (p = 0.0154). The cross-product contribution (2FI) and quadratic model were found to be adequate and statistically accurate with correlation value (R²) of 0.9054 and 0.9450 to predict the drug loading and drug release respectively. An increase in concentration of HPMC and SA decreases the drug loading as well as the drug release. The obtained optimum values of drug loading and DS released were 7.43 % and 85.54 % respectively, which were well in agreement with the predicted value by RSM.     

Determination of Silver with On-Line Preconcentration Using Dithiozone Chelate and Carbon Nanotubes for Preconcentration with Detection by Flame Atomic Absorption Spectrometry

A novel flow injection system incorporating a micro-column packed with carbon nanotubes (CNTs) as an adsorbent has been applied to the on-line preconcentration of trace silver with detection by flame atomic absorption spectrometry. Silver is first chelated by dithizone (H₂Dz), then retained on the CNTs surface and afterward quantitatively eluted by methanol. Influencing parameters, including the concentration of reaction reagent, enrichment variables, and elution variables were investigated. The adsorption mechanisms of Ag-H₂Dz chelate retained onto the CNTs surface have also been studied. By loading 6.9 mL sample solution, a linear calibration graph is obtained within the range of 3–120 µg L^?1 with R of 0.9996, and a detection limit (3σ) of 0.8 µg L^?1 is achieved, along with a precision of 1.6% R.S.D. at the 30 µg L^?1 level (n = 7). The dynamic sorption capacity of CNTs for silver is 122 mg g^?1. The procedure is demonstrated by measurement of spike recovery in a series of water samples, giving rise to spike recoveries in the range of 96.8–99.7%.     

Sorption of Cd(II) onto carbon-based materials—a comparative study

The sorption behaviour of Cd(II) on three carbon-based materials including activated carbon (AC), carbon nanotubes (CNTs) and carbon-encapsulated magnetic nanoparticles (CEMNPs) which were prepared under similar conditions by nitric acid treatment were investigated. Generally, sorption of cadmium on these materials increased with the increase of pH. For AC and CNTs very similar results were obtained, while CEMNPs exhibits much higher affinity for Cd(II) despite of almost the same surface acidity. Thus, cadmium retention on tested sorbents was more dependent on the concentration of specific active sites than the total surface area available. The equilibrium sorption data were better fitted to Langmuir isotherm. The theoretical saturation capacity of the monolayer derived from this model at pH 8.0 for AC, CNTs and CEMNPs are 9.91 mg g^?1, 20.37 mg g^?1 and 91.0 mg g^?1, respectively. The kinetic of Cd(II) sorption is fitted for pseudo-second order equation and could be described as a combination of film diffusion and intra-particle diffusion, whereby the last one dominates. The experimental parameters for preconcentration of cadmium on a microcolumn packed with CEMNPs prior to its determination by flame atomic absorption spectrometry have been investigated. Cadmium can be quantitatively retained at pH 8 from sample volumes up to 150 mL and then eluted completely with 3 mL of 0.5 mol L^?1 HNO₃.     

Complexation of Ketoconazole by Native and Modified Cyclodextrins

Complexation of ketoconazole (KET), a broad-spectrum antifungal drug, with β- and γ-cyclodextrins (CDs), heptakis (2,6-di-O-methyl)-β-CD (2,6-DM-β-CD), heptakis (2,3,6-tri-O-methyl)-β-CD (TM-β-CD), 2-hydroxypropyl-β-CD (2HP-β-CD) and carboxymethyl-β-CD (CM-β-CD) was studied. The stability constants were determined by the solubility method at pH = 6 and for 2,6-DM-β-CD and CM-β-CD at pH = 5. At pH = 6, the stability constants increased in the order: TM-β-D < γ-CD < 2HP-β-CD < β-CD < CM-β-CD < 2,6-DM-β-CD. At pH = 5, due to the increased ionization of KET, the stability constant with CM-β-CD increased and with 2,6-DM-β-CD decreased. For complexes of KET with 2HP-β-CD and 2,6-DM-β-CD, the thermodynamic parameters of complexation were determined from the temperature dependence of the corresponding stability constants. For β–γ and TM-β-CD complexes, calculations using HyperChem 6 software by the Amber force field were carried out to gain some insight into the host–guest geometry.     

Formulation of pH-sensitive aminated chitosan–gelatin crosslinked hydrogel for oral drug delivery

The objective of this study is to develop efficient pH-sensitive hydrogel based on aminated chitosan (AmCs) and gelatin (Gel) biopolymers for oral drug delivery. Herein, AmCs was chemically crosslinked with gelatin (Gel) biopolymer with different ratios, while their structures, thermal profiles and morphological properties were investigated by FTIR, TGA and SEM characterization tools, respectively. Moreover, gel-content, crosslinking density and rheological analysis were also performed. The results clarified that the developed AmCs-Gel crosslinked hydrogel displayed variable pH-sensitive swelling profiles. By increasing AmCs ratio, the swelling ratio was boosted at pH 1.2 and declined at pH 7.4. Besides, by increasing gelatin ratio in the hydrogel matrix, the loading efficiency of Oseltamivir phosphate (as a model of drug) was augmented and reached maximum value of 79.0% by AmCs-Gel (2:3) crosslinked hydrogel. The in vitro drug release profiles were investigated for 6 h in simulated gastric fluid [SGF; pH 1.2] and simulated colon fluid [SCF; pH 7.4]. Variable release profiles were realized depending on variation of AmCs and Gel ratios in the crosslinked hydrogel matrix. Finally, the formulated smart crosslinked AmCs-Gel hydrogels demonstrated acceptable biodegradability with no cellular toxicity, suggesting their applicability as pH-sensitive oral drug carriers.     

New methods for the detection of cyanide based on displacement of the glutathione ligand of glutathionylcobalamin by cyanide

Glutathionylcobalamin (GSCbl) is a vitamin B₁₂ derivative that contains glutathione as the upper axial ligand to cobalt via a Co–S bond. In the present study, we discovered that cyanide reacted with GSCbl, generating cyanocobalamin (CNCbl) and reduced glutathione (GSH) via dicyanocobalamin (diCNCbl) intermediate. This reaction was induced specifically by the nucleophilic attack of cyanide anion displacing the glutathione ligand of GSCbl. Based on the reaction of GSCbl with cyanide, we developed new methods for the detection of cyanide. The reaction intermediate, violet-coloured diCNCbl, could be applied for naked eye detection of cyanide and the detection limit was estimated to be as low as 520 μg L^?1 (20 μM) at pH = 10.0. The reaction product, CNCbl, could be applied for a spectrophotometric quantitative determination of cyanide with a detection limit of 26 μg L^?1 (1.0 μM) at pH = 9.0 and a linear range of 26–520 μg L^?1 (1.0–50 μM). In addition, the other reaction product, GSH, could be applied for a fluorometric quantitative determination of cyanide with a detection limit of 31 μg L^?1 (1.2 μM) at pH = 9.0 and a linear range of 31–520 μg L^?1 (1.2–20 μM). These new GSCbl-based methods are simple, highly specific and sensitive with great applicability for the detection of cyanide in biological and non-biological samples.     

Confinement and controlled release of quinine on chitosan–montmorillonite bionanocomposites

To accomplish the controlled‐release systems based on layered clay minerals, one of the best ways is to intercalate organic molecules into the interlayer gallery of clay minerals. Into a series of chitosan (CS) intercalated montmorillonite (MMT) nanocomposites, prepared via ion‐exchange route, antimalarial drug [quinine (QUI)] was loaded to act as effective drug delivery systems. Among the CS–MMT nanocomposites, higher drug adsorption with decreasing CS concentration was observed. CS–MMT and CS–MMT/QUI intercalated compounds were characterized by powder X‐ray diffraction, Fourier transform infrared spectroscopy, and thermal analysis. The synthesized nanocomposites, filled in the gelatin capsules followed by coating of Eudragit® L 100, were tested for in vitro drug release performance in the sequential buffer environments at 37 ± 0.5 °C. As no drug release (0%) was observed in the gastric fluid, the coating of Eudragit® L 100 to the capsules is highly adequate. However, the drug release rate was comparatively faster from the CS intercalated clay with compare with pure clay. The drug release kinetic data revealed that the release of QUI from the nanocomposites can be explained by modified Freundlich model. © 2011 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem, 2011     

Enhancement of Fluorescence Intensity of Tramadol and Its Main Metabolites in LC Using Pre-Column Derivatization with 9-Fluorenylmethyl Chloroformate

Tramadol was found to exhibit weak fluorescence with a maximum emission at 300 nm when excited at 200 nm. Also, fluorescence spectra of the drug and its two main metabolites, O-desmethyltramadol and N-desmethyltramadol are not practically identical. Thus low and different sensitivities have been reported for the drug and its metabolites in previously published work. In the present method using 9-fluorenylmethyl chloroformate (FMOC-Cl) as labeling agent, equal and magnified fluorescence intensity were obtained for the analytes. The drug, its metabolites and an internal standard (oseltamivir phosphate) were extracted from serum by dichloromethane. Pre-column derivatization of the analytes was achieved using FMOC-Cl in the presence of borate buffer (0.1 M, pH 7.5). Liquid chromatography with a mobile phase consisting of a mixture of 0.05 M phosphate buffer containing triethylamine (2 ml L^?1; pH = 3.0) and methanol (54:46; v/v) and a Shimpack CLC-ODS column were used for analytical separation of the analytes. The fluorescence of the column effluent was monitored at an excitation and emission wavelengths of 265 and 315 nm, respectively. The analytical method was linear over the concentration range of 1.0–1,280 ng mL^?1 of the parent drug and its metabolites and limit of quantification of 1.0 ng mL^?1 was obtained for the analytes using 10 μL injection. The method validation was studied and the validated method applied in a bioequivalence study of 2 different tramadol preparations in 24 healthy volunteers.     

Intercalation and controlled release of vitamin B<Subscript>6</Subscript> from montmorillonite–vitamin B<Subscript>6</Subscript> hybrid

Controlled release of a therapeutic agent to patients is gaining enormous importance during the recent past. The present paper focused on the intercalation of vitamin B₆ (pyridoxine, VB₆) into montmorillonite (MMT) as a controlled release drug carrier. MMT used in this study is of Indian origin. Intercalation of VB₆ into MMT at different times, temperatures, pH values, and initial concentration is illustrated. The MMT–VB₆ hybrid was characterized by X-ray diffraction, Fourier transform infrared, and thermogravimetric analysis. VB₆ was successfully adsorbed on the surface of MMT and also intercalated into the interlayer of MMT. The release processes were monitored under in vitro conditions using simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 7.4) at 37 ± 0.5 °C. In vitro release experiments revealed that VB₆ was released from the MMT–VB₆ hybrid steadily and was pH-dependent.     

Simultaneous Determination of Trans-Cinnamaldehyde and Benzaldehyde in Different Real Samples by Differential Pulse Polarography and Study of Heat Stability of Trans-Cinnamaldehyde

Abstract

A simple, sensitive, and accurate differential pulse polarography method for simultaneous determination of trans-cinnamaldehyde and benzaldehyde in food and drug samples were developed. DC polarography, CV, and coulometric techniques were used for investigation the electrochemical behavior of both compounds. In phosphate buffer (pH = 8.2) and 10% v/v of methanol the differential pulse voltammograms of trans-cinnamaldehyde (?1.05 V) and benzaldehyde (?1.31 V) display reproducible peaks. Under these conditions a strict linearity between both analyte concentrations and their peaks height were observed. The detection limits were calculated to be 2.5 × 10^?8 and 1.2 × 10^?8 M for trans-cinnamaldehyde and benzaldehyde in pH = 8.2, respectively. The relative standard deviations for 1.0 × 10^?6 M of both analytes were 2.04 and 1.18. The heat stability of trans-cinnamaldehyde was studied, and it was found that trans-cinnamaldehyde undergoes a heat-induced decomposition at low temperature (>70°C) to produce benzaldehyde.     

Chromatographic Framework to Determine the Memantine Binding Mechanism on Human Serum Albumin Surface

In this work, the interaction of memantine with human serum albumin (HSA) immobilized on porous silica particles was studied using a biochromatographic approach. The determination of the enthalpy change at different pH values suggested that the protonated group in the memantine–HSA complex exhibits a heat protonation with a magnitude around 65 kJ mol^?1. This value agrees with the protonation of a guanidinium group, and confirmed that an arginine group may become protonated in the memantine–HSA complex formation. The thermodynamic data showed that memantine–HSA binding, for low temperature (<293 K), is dominated by a positive entropy change. This result suggests that dehydration at the binding interface and charge–charge interactions contribute to the memantine–HSA complex formation. Above 293 K, the thermodynamic data ΔH and ΔS became negative due to van der Waals interactions and hydrogen bonding which are engaged at the complex interface. The temperature dependence of the free energy of binding is weak because of the enthalpy–entropy compensation caused by a large heat capacity change, ΔC _p = ? 3.79 kJ mol^?1 K^?1 at pH = 7. These results were used to determine the potential binding site of this drug on HSA.     

Co-delivery of docetaxel and doxorubicin using biodegradable PEG-PLA micelles for treatment of breast cancer with synergistic anti-tumour effects

Poly(ethylene glycol)-poly(lactic acid) copolymer, prepared by ring opening polymerization, was used as a single platform to co-deliver both hydrophilic doxorubicin and hydrophobic docetaxel (DTX) in a simulated physiological environment. The average size of the negatively charged drug loaded polymeric micelles were found to be 293 nm. The drug loading (%) and encapsulation efficiency (%) were calculated to be 1.21 and 59.0, respectively. The in vitro cytotoxicity test using MCF7 breast cancer cells was conducted using 1 × 10⁴ cells in 10% FBS and 1% antibiotic, and the absorbance of formazan was evaluated at 570 nm. Cell growth inhibition by MTT assay showed viability of 33% of the MCF7 cells after treatment with drug-loaded micelles for 48 h. Controlled release of drugs from the polymeric micelles indicated a burst release effect initially; whereas, 98% of drug could be released at pH 7.4 within a time period of 96 h. Time period for drug release shorten to 48 h only in simulated mild acidic pH (5.4) condition. The in vitro drug release study from micelles indicated synergistic cytotoxicity effect in human metastatic breast cancer MCF7 cell.     

Electrochemical synthesis of oxide nanotubes on Ti6Al7Nb alloy and their interaction with the simulated body fluid

The aim of the present work was to investigate electrochemical behavior of the Ti6Al7Nb alloy in the simulated body fluid (SBF) containing Ca²⁺, HCO₃ ^?, and HPO₄ ^2? ions. At first, optimal conditions necessary for oxide nanotube formation were determined. The experiments were conducted in the 1 M (NH₄)₂SO₄ with 0.5 wt% NH₄F electrolyte at room temperature. Anodization of the alloy samples was carried out under variable external voltage U in the range from 10 to 40 V at room temperature. Obtained surface morphology was examined by SEM and X-ray techniques. Nanotube diameter was calculated and correlated with the imposed voltage. Having control over the size of nanotubes, samples with the obtained nanostructures of a chosen diameter were immersed into SBF solution with pH = 7.4 for a fixed period of time. Then, they were removed from the fluid and subjected to the electrochemical investigation. Corrosion current and corrosion potential were determined, and it was found that the best anticorrosion properties were obtained for heat-treated nanotube layer: i _corr = 39 nA/cm² and E _corr = ?0.236 V vs Ag/AgCl. Finally, the interaction between the oxide surface and the solution was studied using polarization and electrochemical impedance spectroscopy (EIS) techniques.     

SDS-Based Biomembrane Mimetic Chromatography for Prediction of Human Drug Transport as an in Vitro Technique

The main oral drug absorption barriers are fluid cell membranes, and generally drugs are absorbed by a passive diffusion mechanism. On the other hand, the blood–brain barrier (BBB) is considered to be the main barrier to drug transport into the central nervous system (CNS). The BBB restricts the passive diffusion of many drugs from blood to brain. Biopartitioning micellar chromatography (BMC), a mode of micellar liquid chromatography that uses micellar mobile phases in adequate experimental conditions, can be useful as an in vitro system in mimicking the drug partitioning process into biological systems. In this study, relationships between the BMC retention data of a heterogeneous set of 12 drugs and their pharmacokinetics parameters (human oral drug absorption and BBB penetration ability) are studied and the predictive ability of the models is evaluated. Modeling of log k _BMC of these compounds was established by multiple linear regression in two different concentrations (0.07 and 0.09 M) of sodium dodecyl sulfate (SDS). The results showed a fair correlation between human oral drug absorption and BMC retention data in 0.09 M SDS (R ² = 0.864) and a good correlation between the blood–brain distribution coefficient and BMC retention data in 0.07 M of SDS (R ² = 0.887). Application of the developed models to a prediction set demonstrated that the model is also reliable with good predictive accuracy. The external and internal validation results showed that the predicted values are in good agreement with the experimental value.     

Encapsulation of complementary model drugs in spray-dried nanostructured materials

Two model drugs of different physico-chemical and pharmaceutical properties (ibuprofen, acetaminophen) have been incorporated together or separately in silica-based microspheres using sol–gel and spray-drying processes. A variable amount of a neutral surfactant Brij-56© has also been added. The properties of the microspheres vary significantly depending on their composition. Three kinds of texture are identified: (1) silica containing spheroid nano-domains (formed by ibuprofen; diameters between 20 and 100 nm), (2) silica containing worm-like mesophases (formed by Brij-56© and both model drugs, typical correlation distances ~6 nm), (3) silica intimately mixed with the drug (acetaminophen) without visible phase-separation. The kinetics of drug release in simulated intestinal fluid strongly depend on these textures. The association of ibuprofen and acetaminophen in a single type of microsphere and without surfactant favours a concomitant release. Possible mechanisms of materials’ formation are discussed.     

Solubilization and Release of a Model Drug Nimesulide from PEO–PPO–PEO Block Copolymer Core–Shell Micelles: Effect of Size of PEO Blocks

The commercially available polypropylene oxide (PPO)–polyethylene oxide (PEO) symmetrical triblock copolymers (Pluronics^®) have been recognized as pharmaceutical excipients and used in a variety of applications. This paper reports studies on micellar and solubilization behavior of three PEO–PPO–PEO block copolymers, viz. P103, P104 and P105 (same PPO mol. wt = 3250 g·mol^?1 but different  % PEO = 30, 40 and 50 %, respectively) in aqueous solutions. Critical micellization concentrations (CMCs), critical micellization temperatures (CMTs), and micelle size/polydispersity for copolymers with and without the drug, nimesulide (NIM), are reported. The solubilization of NIM is significantly enhanced with increasing hydrophobicity (P103 > P104 > P105), concentration, temperature and in the presence of added salt. The copolymer hydrophobicity, temperature and the drug loading strongly affect micelle behavior. The micelle–water partition coefficient (P) and thermodynamic parameters of solubilization, viz. Gibbs energy ( $ \Updelta G_{s}^{\text{o}} $ ), enthalpy ( $ \Updelta H_{s}^{\text{o}} $ ) and entropy ( $ T\Updelta S_{s}^{\text{o}} $ ), were calculated. The solubilization site of the drug in different micellar solutions and its release from Pluronics^® micelles in phosphate buffer saline (PBS) solution at 37 °C were examined. The kinetics of NIM exhibits burst release characteristics, which are believed to be controlled by degradation of the copolymers. These studies were carried out to investigate the feasibility of using Pluronics^® as a release vehicle of nimesulide in vitro. From the results, it was concluded that Pluronic^® based formulations might be practical for drug delivery.     

Optimization of Capillary Isotachophoretic Method for Histidine Determination in Protein Matrices

The capillary isotachophoretic method was optimized and used for histidine determination in food samples. The optimum conditions for histidine separation and determination were found on the experimental conditions such as: selectivity, separation speed, pH, concentration of the leading and terminating electrolytes, and electroosmotic flow additives. The optimum electrolytes composition [leading electrolyte: 7 mM NH₄OH + 15 mM 2-(N-morpholino)ethanesulfonic acid + 1% hydroxyethylcellulose; pH = 6.10 and terminating electrolyte: 15 mM aminocaproic acid +5 mM acetic acid +40% methanol; pH = 5.10] and conditions of analysis were adopted for histidine determination in food samples (meat and fish products). The proposed electrolyte system was characterized by linearity (10–100 and 100–430 mg · L^?1 with R² = 0.9976 and 0.9991), accuracy (99.5% and 98%), intra-assay of the relative step height (1.40% for standard and 3.20% for food samples analysis), inter-assay of the relative step height (3.65% and 6.30%) and satisfactory quantification and detection limits. The obtained results were compared to a chromatographic method (reversed-phase (RP)-HPLC) for determination of histidine. The average concentrations of histidine in the samples assayed by both methods were statistically comparable. It should be noted that the proposed histidine determination method can be considered as a contribution to Green Analytical Chemistry.     

pH-controlled morphological structure and electrochemical performances of polyaniline/nickel hexacyanoferrate nanogranules during electrochemical deposition

To explore the dependences of morphology and electrochemical performance of polyaniline/nickel hexacyanoferrate (PANI/NiHCF) nanogranules on pH value of the reaction system, electrodeposition of PANI/NiHCF nanogranules was performed across a pH range from 0 to 7 on carbon nanotubes (CNTs)-modified platinum substrate by cyclic voltammetry in a mixture of 0.002 mol L^?1 NiSO₄, 0.25 mol L^?1 Na₂SO₄, 0.002 mol L^?1 K₃Fe(CN)₆, and 0.01 mol L^?1 aniline solutions. The morphology and structure of PANI/NiHCF nanogranules were characterized by scanning electron microscopy (SEM) and Fourier transform infrared (FTIR) spectroscopy, respectively. The supercapacitive performances of the nanogranules were investigated with cyclic voltammetry (CV), charge/discharge tests, and electrochemical impedance spectroscopy (EIS). The results showed that the nanogranules with different morphology and sizes were obtained with the change of pH values from 0 to 7, which could control the mechanism of homogeneous or heterogeneous nucleation directly. The nanogranules were dispersed in matrix uniformly at pH 0 and pH 1, while the size of which decreased with the increase of pH values. The smooth cross-linking network structure was found from pH 2 to 7. The structure of PANI/NiHCF nanogranules had slightly changed from pH 0 to 7. PANI/NiHCF nanogranules had good electrochemical performance from pH 0 to 7 in a mixture of 0.5 mol L^?1 H₂SO₄ and 0.5 mol L^?1 KNO₃ solutions, and the highest specific capacitance value of 274 F g^?1 was obtained at current densities of 2 mA cm^?2 in neutral medium. PANI/NiHCF nanogranules had high stability in neutral medium after 2,000 cycles by CV.     

Performances of NaCS–WSC protein drug microcapsules with different degree of substitution of NaCS using sodium polyphosphate as cross-linking agent

Sodium cellulose sulfate–water soluble chitosan (NaCS–WSC) microcapsules loaded with lactoferrin were fabricated with special performances using different degree of substitution (DS) of NaCS and WSC as potential micro-drug-carriers for colon. Effect of using cross-linking agent (sodium polyphosphate) and DS of NaCS on the structures and performances of microcapsules was studied. The results of laser scanning confocal microscope showed that fluorescein isothiocyanate-labeled lactoferrin distributed evenly in the drug-loaded microcapsules with cross-linker. NaCSs (DS: 0.51 and DS: 0.66, respectively) were chosen to prepare lactoferrin loaded microcapsules with WSC and cross-linker for comparison studies. DS of NaCS had some effects on erosion properties in which the erosion ratios of microcapsules with DS of 0.51 were higher than that with DS of 0.66, but showed no effect on swelling behaviors. Drug loading and encapsulation efficiencies of microcapsules (DS: 0.66) were 51.05 ± 0.97 and 75.88 ± 1.44 %, respectively, which were higher than that of microcapsules with DS of 0.51. In vitro release studies showed that the percentage of drug release of microcapsules (DS: 0.51) were higher than that of microcapsules with DS of 0.66 in simulated colonic fluid (pH 6.4) under mechanism of Anomalous (non-Fickian) transport, indicating that they are promising candidates as sustained protein drug delivery carriers with special performances.