Development and evaluation of pH-sensitive biodegradable ternary blended hydrogel films (chitosan/guar gum/PVP) for drug delivery application

AbstractpH responsive hydrogels have gained much attraction in biomedical fields. We have formulated ternary hydrogel films as a new carrier of drug. Polyelectrolyte complex of chitosan/guar gum/polyvinyl pyrrolidone cross-linked via sodium tripolyphosphate was developed by solution casting method. Fourier transform infrared spectroscopy, scanning electron microscopy and thermogravimetric analysis were conducted to examine the interactions between the polymeric chains, surface morphology and thermal stability, respectively. The swelling tests resulted that the swelling was reduced with the increase in the concentration of crosslinker due to the more entangled arrangement and less availability of pores in hydrogels. Ciprofloxacin hydrochloride was used as a model drug and its release in simulated gastric fluid, simulated intestinal fluid and phosphate buffer saline solution was studied. pH responsive behaviour of the hydrogels have subjected these hydrogels for drug release applications.

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FABRICATION OF CURCUMIN LOADED GUAR GUM MICROPARTICLES FOR CONTROLLED RELEASE BY EMULSION GELATION TECHNIQUE

INDIAN DRUGS ◽

10.53879/id.54.02.10758 ◽

2017 ◽

Vol 54 (02) ◽

pp. 69-72

Author(s):

G Roopa ◽

◽

C. Jayanthi ◽

R Karki ◽

H. Joshi ◽

...

Keyword(s):

Particle Size ◽

Controlled Release ◽

Guar Gum ◽

Drug Loading ◽

Surface Characteristics ◽

Gastric Fluid ◽

Simulated Gastric Fluid ◽

Simulated Intestinal Fluid ◽

Dsc Studies

Cross-linked guar gum microparticles of curcumin were prepared for controlled release by emulsion gelation method using glutaraldehyde as cross-linking agent. Morphology and surface characteristics of the formulations were assessed by scanning electron microscopy. Particle size of the guar gum microparticles was determined by optical microscopy. The mean particle size ranged from 82 to 250 μ. The % drug loading was found to be in the range of 20 to 51% while the percentage encapsulation efficiency was ranging between 29 to 86%. FT-IR and DSC studies revealed the compatibility of the drug with the polymer. Formulation CGMP3 exhibited maximum % EE of 84%, In vitro drug-release studies were performed in simulated gastric fluid (without enzymes) for 2 h followed by simulated intestinal fluid (without enzymes) for 6 h and continued for 24 h. Formulation CGMP3 exhibited relatively more sustained release profile than the other formulations. All formulations of 1.5% guar gum (CGMP2, CGMP3 and CGMP4) have shown retarded release than 1.0 % guar gum formulations (CGMP6, CGMP7 and CGMP8). Optimal glutaraldehyde concentration was found to be 2%. The optimized formulation subjected to stability studies was found to be stable when observed for particle size and drug content.

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

Molecules ◽

10.3390/molecules26020449 ◽

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.

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Fabrication of Multi-Layered Microspheres Based on Phase Separation for Drug Delivery

Micromachines ◽

10.3390/mi12060723 ◽

2021 ◽

Vol 12 (6) ◽

pp. 723

Author(s):

He Xia ◽

Ang Li ◽

Jia Man ◽

Jianyong Li ◽

Jianfeng Li

Keyword(s):

Aqueous Solution ◽

Phase Separation ◽

Gastric Fluid ◽

Simulated Gastric Fluid ◽

Sustained Drug Release ◽

Simulated Intestinal Fluid ◽

Glycol Diacrylate ◽

Emulsion Droplets ◽

Collection Tube ◽

Poly Ethylene

In this work, we used a co-flow microfluidic device with an injection and a collection tube to generate droplets with different layers due to phase separation. The phase separation system consisted of poly(ethylene glycol) diacrylate 700 (PEGDA 700), PEGDA 250, and sodium alginate aqueous solution. When the mixture droplets formed in the outer phase, PEGDA 700 in the droplets would transfer into the outer aqueous solution, while PEGDA 250 still stayed in the initial droplet, breaking the miscibility equilibrium of the mixture and triggering the phase separation. As the phase separation proceeded, new cores emerged in the droplets, gradually forming the second and third layers. Emulsion droplets with different layers were polymerized under ultraviolet (UV) irradiation at different stages of phase separation to obtain microspheres. Microspheres with different layers showed various release behaviors in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF). The release rate decreased with the increase in the number of layers, which showed a potential application in sustained drug release.

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Preparation and Characterization of Cefradine/Montmorillionite Composites

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.560-561.434 ◽

2012 ◽

Vol 560-561 ◽

pp. 434-437 ◽

Cited By ~ 1

Author(s):

Lan Wang ◽

Wen Ji Guo ◽

Yan Zhao Zhao

Keyword(s):

Gastric Fluid ◽

Simulated Gastric Fluid ◽

X Ray Diffraction ◽

Simulated Intestinal Fluid ◽

Solution Intercalation ◽

Method Of Solution ◽

Ft Ir ◽

In The Beginning ◽

Ft Ir Spectroscopy

The objective of this paper was to prepare the composite of crefradine/montmorillionite in the method of solution intercalation. The drug load and intercalation rate varied with the drug concentration. X-ray diffraction (XRD), Fourier transformed infrared (FT-IR) Spectroscopy, and thermal analysis (TG-DSC) were applied to characterize composite mentioned above. Together with drug release tests, results indicate cefradine intercalated into montmorillionite.The release profiles of cefradine/MMT in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 7.4) at 37°Cduring 10h are shown in Fig. 4. The amount of cefradine in the beginning 2h came up to 35% and 50%, and in the following time, cefradine released slowly. The release behaviors met the requirements of sustained release.

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

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i11.24366 ◽

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.

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Release Activity of Encapsulated Lactobacillus plantarum NBRC 3070 in Optimum Alginate - Aloe vera Matrices during Simulated Gastric Fluid (SGF) and Simulated Intestinal Fluid (SIF) Exposure

Asian Journal of Applied Sciences ◽

10.24203/ajas.v5i2.4500 ◽

2017 ◽

Vol 5 (2) ◽

Author(s):

Nur Syahirah Sallehudin ◽

Khalilah Abdul Khalil ◽

Maslinda Musa ◽

Hifa Nazirah Mohd Yazid ◽

Anida Yusof

Keyword(s):

Aloe Vera ◽

Clinical Results ◽

Gastric Fluid ◽

Alginate Beads ◽

Simulated Gastric Fluid ◽

Intestinal Fluid ◽

Simulated Intestinal Fluid ◽

Encapsulated Cells ◽

Aloe Vera Gel ◽

Encapsulation Process

Probiotic encapsulation approach has the potential to protect microorganisms and to deliver them into the gut. Because of the promising preclinical and clinical results, probiotics have been incorporated into a range of products. However, there are still many challenges to overcome with respect to the encapsulation process and the conditions prevailing in the gut. Thus in this study, the release activity of encapsulated L. plantarum NBRC 3070 and Aloe vera gel within alginate coated chitosan matrices during simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) exposure were investigated. There were four groups of beads prepared in this study: 1) Encapsulated probiotic and Aloe vera within alginate beads (chitosan coated), 2) Encapsulated probiotic within alginate beads (chitosan coated), 3) Encapsulated probiotic and Aloe vera within alginate beads (uncoated) and 4) Encapsulated probiotic alone within alginate beads (uncoated). Encapsulation process was carried out using extrusion method. The optimized composition of alginate matrix (1.34% w/v) and Aloe vera gel (1.99% w/v) were used.Â In order to investigate their release activity, all beads were exposed in Simulated Gastric (SGF) at pH 2.5 and Simulated Intestinal Fluids (SIF) at pH 6.5 for 120 min and 270 min, respectively. Based on the findings, alginate-Aloe vera beads with chitosan coated was able to protect L. plantarum NBRC 3070 during SGF exposure with only 1 log10 cfu/mL reduction. The presence of Aloe vera gel in the beads improved the survivability of the cells. Encapsulated cells were observed successfully slow released of cells from the beads after exposure in SIF. Scan Electron Microscope (SEM) result had shown that cross link activity of the optimum alginate-Aloe vera with chitosan coating resulted in better survival of cells after simulated gastro and able to deliver sufficient probiotic dose to intestinal region. The combinations were able to improve encapsulated cells survivability during low acidic environment passage and release activity into the intestinal target region.Â Â

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Survival Survey of Lactobacillus acidophilus In Additional Probiotic Bread

Turkish Journal of Agriculture - Food Science and Technology ◽

10.24925/turjaf.v7i4.588-592.2247 ◽

2019 ◽

Vol 7 (4) ◽

pp. 588

Author(s):

Truong Duc Thang ◽

Le Thi Hanh Quyen ◽

Hoang Thi Thuy Hang ◽

Nguyen Thien Luan ◽

Dang Thi KimThuy ◽

...

Keyword(s):

Lactobacillus Acidophilus ◽

Xanthan Gum ◽

Gastric Fluid ◽

Probiotic Bacteria ◽

Simulated Gastric Fluid ◽

Protective Agent ◽

Intestinal Fluid ◽

Simulated Intestinal Fluid ◽

The World ◽

Alginate Matrix

Bread is a popular food in the world because of its variety and convenience. Currently, studies on the adding probiotics to bread are limited due to the adverse effects of processing, such as baking temperature, aerobic environment to the probiotic bacteria. The objective of this study was to produce probiotic cream bread, in which Lactobacillus acidophilus was microencapsulated with Alginate 2% (A); Alginate 2% + maltodextrin 1% (AM); Alginate 2% + xanthan gum 0.1% (AX); and Alginate 2% + maltodextrin 1% + xanthan gum 0.1% (AMX). Microcapsules were added to the kernel, conducting encapsulation yield investigations, survival in baking, preservation of bread, and in simulated gastric fluid and simulated intestinal fluid conditions after 8 days of storage. The results showed that the addition of xanthan gum enhanced the encapsulation yield, it reached 92.9% and 92.37% in AMX and AX samples, respectively. The viability of L. acidophilus during baking was decreased by 3.64 and 3.75 Log (CFU/bread) in AMX and AM samples, compared to A and AX which were decreased by 4.75 and 4.44 Log (CFU/ bread). In SGF (Simulated Gastric Fluid) and SIF (Simulated Intestinal Fluid) conditions, the AMX microcapsules provide the best probiotic protection among the four tested carriers. The combination of xanthan gum and maltodextrin in alginate matrix, eventually leading to having dual efficiency: First, xanthan gum would act as buffers that reduce acid activity; Second, maltodextrin acting as a protective agent of L. acidophilus against high temperature as well as potential prebiotic that improve the viability of probiotic.

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IN VITRO RELEASE STUDIES OF CARBAMAZEPINE TABLETS AND BENZOYL METRONIDAZOLE SUSPENSIONS USING THE FLOW-THROUGH CELL APPARATUS AND SIMULATED GASTROINTESTINAL FLUIDS

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2017v9i4.18929 ◽

2017 ◽

Vol 9 (4) ◽

pp. 54 ◽

Cited By ~ 3

Author(s):

Jose Raul Medina ◽

Jonathan Hernandez ◽

Marcela Hurtado

Keyword(s):

In Vitro Release ◽

Gastric Fluid ◽

Simulated Gastric Fluid ◽

Dissolution Time ◽

Intestinal Fluid ◽

Simulated Intestinal Fluid ◽

Release Studies ◽

Flow Through ◽

Vitro Release

Objective: To characterize the in vitro release of carbamazepine tablets and benzoyl metronidazole suspensions using the flow-through cell apparatus and simulated gastrointestinal fluids.Methods: Tegretol® tablets, Flagyl® suspension, and generic formulations of each were tested. Release studies were performed using an automated flow-through cell apparatus. Simulated gastric fluid (with and without pepsin) and simulated intestinal fluid (without pancreatin) at 16 ml/min and fasted state simulated intestinal fluid at 8 ml/min, all at 37.0±0.5 °C, were used as dissolution media. The quantity of dissolved carbamazepine and benzoyl metronidazole was determined at 5-min intervals until 60 min at 285 and 278 nm, respectively. Percentage dissolved at 60 min, mean dissolution time, dissolution efficiency values, and t10%, t25%, t50% and t63.2% were calculated. Mean values for all parameters were compared between the reference and generic formulations using Studentʼs t-test. Dissolution data were fitted to different kinetic models.Results: Simulated gastric fluid without pepsin showed no discriminative capability for carbamazepine tablets. Significant differences were observed between the reference and generic formulations for almost all parameters (*P<0.05). In some cases, the logistic model best described the in vitro release of both drugs.Conclusion: Using an apparatus and media that best simulates the gastrointestinal environment, we identified differences in the rate and extent of dissolution of both drugs that could help to optimise the design of interchangeable formulations. Based on the physicochemical characteristics of carbamazepine and benzoyl metronidazole and the conditions in which the formulations were tested, these differences could be of clinical relevance.

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INCORPORATION OF VITAMIN E ONTO CROSS-LINKED GALACTOMANNAN PHOSPHATE MATRIX AND IN VITRO STUDY

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i5.24645 ◽

2018 ◽

Vol 11 (5) ◽

pp. 355 ◽

Cited By ~ 1

Author(s):

Juliati Br Tarigan ◽

Djendakita Purba ◽

Cut Fatimah Zuhra

Keyword(s):

Vitamin E ◽

In Vitro Study ◽

Gastric Fluid ◽

Simulated Gastric Fluid ◽

Crosslinking Reaction ◽

Reliability Study ◽

Simulated Intestinal Fluid ◽

Palm Fatty Acid Distillate ◽

The Fourier Transform

Objective: This study demonstrated the incorporation of Vitamin E from palm fatty acid distillate onto crosslinked galactomannan phosphate (CGP) matrix.Methods: CGP was obtained from the crosslinking reaction of galactomannan from Arenga pinnata (GAP) with tri-sodium metaphosphate (TMF) ranging from 1:1 to 4:3 while incorporation of Vitamin E was conducted in two steps to form films. The reliability study of Vitamin E in CGPVE was conducted using a solution of pepsin and sodium chloride and also in solution of pancreatin and buffer phosphate.Results: The Fourier-transform infrared spectrum indicated the presence of phosphate in CGP while the scanning electron microscope images depicted the changes of surface morphology from smooth (GAP) to rough and hollow (CGP) which confirmed that crosslink had occurred. The swelling study of CGP showed that the swelling indexes were similar and decreased with the increase of TMF. The efficiency of CGP to absorb Vitamin E ranged from 89.66% to 91.09%. The in vitro releasing study of Vitamin E in simulated gastric fluid and simulated intestinal fluid showed that only a small amount of Vitamin E was released.Conclusions: This study demonstrated that CGP can be prepared and is potentially useful for drug delivery to the colon.

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Naturally Derived Matrix for Controlled Selenium Nanoparticles Delivery

Key Engineering Materials ◽

10.4028/www.scientific.net/kem.695.284 ◽

2016 ◽

Vol 695 ◽

pp. 284-288 ◽

Cited By ~ 1

Author(s):

Simona Cavalu ◽

Vasile Laslo ◽

Florin Banica ◽

Simona Ioana Vicas

Keyword(s):

Gastric Fluid ◽

Point Of View ◽

Matrix Composition ◽

In Vitro Dissolution ◽

Simulated Gastric Fluid ◽

Elemental Selenium ◽

Simulated Intestinal Fluid ◽

Advantages And Disadvantages ◽

Probiotic Lactic Acid Bacteria

The aim of this study is to develop a lyophilized matrix (microspheres) as a controlled delivery system for nanoselenium particles, using different formulation based on alginate or agar. Elemental selenium is considered as the least toxic of all selenium forms and in the same time supplementation with its nanosize particles has the same or better bioavailability compared to its salts. In our study, nanosized elemental selenium was obtained by fermentation technology using probiotic lactic acid bacteria (Lactobacillus casei). The microspheres have been characterized from structural point of view by using different techniques: FTIR spectroscopy, X-ray Diffraction and SEM. Each individual natural polymer has its own characteristic advantages and disadvantages; it is commonly accepted that naturally derived matrix often show an excellent balance between the mechanical properties, swelling and dissolution capacity. The optimized formulation was proposed upon in vitro dissolution study using Diferential Pulsed Voltammetry in order to measure the concentration of selenium released in simulated gastric fluid (pH=1.2) and simulated intestinal fluid (pH=8.1). The cumulative release of selenium from different formulations showed large differences with respect to matrix composition. We demonstrated that both alginate and agarose-based formulations are suitable to be used in basic environment such as small or large intestine. The results might be of high importance as absorption of selenium occurs mainly in the duodenum, caecum and colon (more than 85%).

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