scholarly journals Improvement in Entrapment Efficiency and In Vitro Digestion Stability of Lutein by Zein Nanocarriers with Pepsin Hydrolysis

2020 ◽  
Vol 2020 ◽  
pp. 1-9 ◽  
Author(s):  
Yan Jiao ◽  
He Han ◽  
Ying Chang ◽  
Dajing Li ◽  
Asad Riaz
Keyword(s):  
Structural Characteristics ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
In Vitro Digestion ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Average Particle ◽  
Simulated Intestinal Fluid ◽  
Bioactive Ingredients

Zein is one of the popular bioactive carriers and play critical roles in the promotion of stability, absorption, and utilization of the nutrients and bioactive ingredients. The application of zein delivery systems for the encapsulation of bioactive ingredients has recently gained increasing interest. The aim of this work was to modify zein by pepsin and prepare the lutein-loaded zein nanoparticle (LZN) and the lutein-loaded zein hydrolysate nanoparticle (LZHN), respectively. The effects of zein hydrolysation on entrapment efficiency and in vitro digestion stability of lutein were also evaluated in this study. Hydrolysation of zein by the pepsin has important effects on lutein embedding. The optimal hydrolysis conditions, including the pepsin concentration (1.5%), temperature (55°C), and time (4 h), enhanced the entrapment efficiency (EE) of lutein by 93.82 ± 2.82% as compared to 85.18 ± 3.28% of the untreated zein, respectively. In contrast to LZN, LZHN had better structural characteristics, the average particle size decreases from 158.40 ± 3.22 nm to 112.2 ± 1.56 nm, and LZHN showed better dispersivity and zeta potential. The stability and release assays in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) showed that hydrolyzed zein nanocarriers by pepsin improved the digestion stability and promoted the release of lutein under gastrointestinal digestive conditions. These results suggest that hydrolyzed zein with pepsin may act as an effective carrier for lutein delivery and shows many potential advantages compared with the zein.

scholarly journals FORMULATION AND EVALUATION OF EXTENDED RELEASE PELLETS OF PIOGLITAZONE HYDROCHLORIDE USING NATURAL AND SYNTHETIC POLYMERS BY FLUIDIZED BED COATING TECHNIQUE

2019 ◽  
pp. 438-446
Author(s):  
GOWTHAMI B ◽  
NIHITHA S ◽  
SANTHI PRIYA NAGAM ◽  
RAMA RAO NADENDLA
Keyword(s):  
Fluidized Bed ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Synthetic Polymers ◽  
Lag Phase ◽  
Average Particle ◽  
Simulated Intestinal Fluid ◽  
Coating Technique ◽  
Fluidized Bed Coating

Objective: The objective of the current work was to develop Pioglitazone hydrochloride (HCl) pellets coated with natural polymer extracted from peas gum and also to compare the drug release profile with coatings containing semi-synthetic and synthetic polymers. Methods: Fluidized bed coating technique was used to develop pellets. A 22 factorial design was employed to study the effect of independent variables (inlet air temperature and spray rate), on dependent variables (percentage entrapment efficiency, percentage friability, and average particle size). Optimization was done by fitting experimental data to the software program. Obtained pellets were subjected to different evaluation parameters which are critical in the development of the dosage form. An in vitro lag phase study was carried out for all batches in simulated gastric fluid (0.1N HCl) for 5 h and in vitro drug release study was carried out for optimized batch (E-2 and P-3) in simulated intestinal fluid (pH 7.4 phosphate buffer). Results: The optimized batches E-2 and P-3 showed satisfactory percentage entrapment efficiency of 92.66±1.52, percentage friability of 0.57±0.03, and average particle size of 1424±16 μm. All batches maintained lag phase for 5 h in 0.1N HCl. An optimized batch of two different sizes exhibited a burst release within 30 min in a simulated intestinal fluid with no significant difference in release rate constant (*p>0.05) and followed first-order kinetics. Conclusion: Thus, Pioglitazone HCl pulsatile pellets were successfully developed for treating diabetes mellitus by fluidized bed coating technique employing factorial design.

scholarly journals PREPARATION AND EVALUATION OF CONTROLLED RELEASE FLOATING MICROSPHERES OF REPAGLINIDE: OPTIMIZATION AND IN-VITRO STUDIES

2017 ◽  
Vol 10 (3) ◽  
pp. 103 ◽  
Author(s):  
Megha Sharma ◽  
Seema Kohli ◽  
Abhisek Pal
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Kinetic Studies ◽  
Entrapment Efficiency ◽  
Gastric Fluid ◽  
Appreciable Amount ◽  
Average Particle

ABSTRACTObjective: To develop and evaluate floating microspheres of repaglinide (RG).Materials and Methods: RG loaded noneffervescent microspheres of different ratios of ethylcellulose (EC) and hydroxypropyl methylcellulose (HPMCK4M) were prepared using polyvinyl alcohol as emulsifier by solvent evaporation technique. Various process variables such as polymer ratio, stirringspeed, concentration of drug, and emulsifying agent were studied. Compatibility of drug and polymers was studied by Fourier-transform infraredspectroscopy (FTIR). Characterization, in-vitro evaluation, and kinetic studies were performed.Results: FTIR spectra have revealed no drug-excipient incompatibility. The average particle size of microspheres was in the range of 312-359 μm. Theresults showed that floating microspheres were successfully prepared with good yield (56.15-64.3%), high entrapment efficiency (58.22-70.14%),and good floating behavior (63.1-76.2%), respectively. In-vitro release data indicates appreciable amount of drug is released (62.28-73.27%) from themicrospheres in gastric fluid. The mechanism of drug release founds to follow first order kinetics (r2=0.986).Conclusion: The developed floating microspheres of RG may be used for prolonged drug release for at least 12 hrs, thereby improving bioavailabilityand patient compliance.Keywords: Repaglinide, Compatibility, Kinetic, Ethylcellulose.

Enhanced oral bioavailability of nisoldipine-piperine-loaded poly-lactic-co-glycolic acid nanoparticles

2017 ◽  
Vol 6 (6) ◽  
pp. 517-526 ◽  
Author(s):  
Permender Rathee ◽  
Anjoo Kamboj ◽  
Shabir Sidhu
Keyword(s):  
Oral Bioavailability ◽  
Drug Loading ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Pharmacokinetic Interaction ◽  
Precipitation Method ◽  
Pharmacokinetic Studies ◽  
Average Particle

AbstractBackground:Piperine helps in the improvement of bioavailability through pharmacokinetic interaction by modulating metabolism when administered with other drugs. Nisoldipine is a substrate for cytochrome P4503A4 enzymes. The study was undertaken to assess the influence of piperine on the pharmacokinetics and pharmacodynamics of nisoldipine nanoparticles in rats.Methods:Optimization studies of nanoparticles were performed using Taguchi L9 orthogonal array, and the nanoparticles were formulated by the precipitation method. The influence of piperine and nanoparticles was evaluated by means of in vivo kinetic and dynamic studies by oral administration in rats.Results:The entrapment efficiency, drug loading, ζ potential, and average particle size of optimized nisoldipine-piperine nanoparticles was 89.77±1.06%, 13.6±0.56%, −26.5 mV, and 132±7.21 nm, respectively. The in vitro release in 0.1 n HCl and 6.8 pH phosphate buffer was 96.9±0.48% and 98.3±0.26%, respectively. Pharmacokinetic studies showed a 4.9-fold increase in oral bioavailability and a >28.376±1.32% reduction in systemic blood pressure by using nanoparticles as compared to control (nisoldipine suspension) in Wistar rats.Conclusion:The results revealed that piperine being an inhibitor of cytochrome P4503A4 enzymes enhanced the bioavailability of nisoldipine by 4.9-fold in nanoparticles.

scholarly journals Water-Dispersible Phytosterol Nanoparticles: Preparation, Characterization, and in vitro Digestion

2022 ◽  
Vol 8 ◽  
Author(s):  
Ao Li ◽  
Aixia Zhu ◽  
Di Kong ◽  
Chunwei Wang ◽  
Shiping Liu ◽  
...  
Keyword(s):  
Particle Size ◽  
Soybean Lecithin ◽  
Average Particle Size ◽  
Soy Protein Isolate ◽  
In Vitro Digestion ◽  
Bimodal Distribution ◽  
Average Particle ◽  
Food Ingredients ◽  
The Impact

For improving solubility and bioaccessibility of phytosterols (PS), phytosterol nanoparticles (PNPs) were prepared by emulsification–evaporation combined high-pressure homogenization method. The organic phase was formed with the dissolved PS and soybean lecithin (SL) in anhydrous ethanol, then mixed with soy protein isolate (SPI) solution, and homogenized into nanoparticles, followed by the evaporation of ethanol. The optimum fabrication conditions were determined as PS (1%, w/v): SL of 1:4, SPI content of 0.75% (w/v), and ethanol volume of 16 ml. PNPs were characterized to have average particle size 93.35 nm, polydispersity index (PDI) 0.179, zeta potential −29.3 mV, and encapsulation efficiency (EE) 97.3%. The impact of temperature, pH, and ionic strength on the stability of fabricated PNPs was determined. After 3-h in vitro digestion, the bioaccessibility of PS in nanoparticles reached 70.8%, significantly higher than the 18.2% of raw PS. Upon freeze-drying, the particle size of PNPs increased to 199.1 nm, resulting in a bimodal distribution. The solubility of PS in water could reach up to 2.122 mg/ml, ~155 times higher than that of raw PS. Therefore, this study contributes to the development of functional PS-food ingredients.

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 DERMAL DELIVERY OF DOCETAXEL LOADED NANO LIQUID CRYSTALS FOR THE TREATMENT OF SKIN CANCER

2019 ◽  
pp. 188-193 ◽  
Author(s):  
ARTI MAJUMDAR ◽  
NIDHI DUBEY ◽  
NITIN DUBEY
Keyword(s):  
Liquid Crystals ◽  
Skin Cancer ◽  
Zeta Potential ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Cell Uptake ◽  
Diffusion Method ◽  
Average Particle ◽  
Uptake Study

Objective: The aim of the present study is to develop docetaxel-loaded nano liquid crystals (NLCs) to enhanced and effective delivery of the drug to the skin cancer. Methods: NLCs bearing docetaxel were prepared by an emulsification solvent diffusion method. The formulated NLCs were characterized for average particle size, polydispersity index (PDI) Zeta potential, entrapment efficiency and in vitro drug release study. The prepared formulations were studied for it's in vitro cell line and cell uptake study. Results: It was revealed that the average size of NLCs was found 178.3±5.07, PDI was 0.189, percent entrapment efficiency was found 71.3±2.49 and Zeta potential was found-17.3±2.4. In vitro release determined by Franz diffusion cell was found 61.6±3.2% after 72 hr. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay shows that Docetaxel loaded NLCs were giving more cytotoxicity as compared to the plain drug. The cell uptake study was found enhanced uptake of fluorescein isothiocyanate (FITC) loaded NLCs in comparison to plain FITC. Docetaxel and docetaxel-loaded NLCs showed 28.3±0.3 and 39.3±1.3 growth inhibition respectively after 48h upon incubation at 0.5 µg/ml concentration (p<0.05). Conclusion: The result of the studies was concluded that NLCs can be used as impending drug delivery system which may enhance the drug uptake and maintain the drug level for longer period of time and it is potential carrier system which can be used for the treatment of skin diseases like cancer.

scholarly journals Development and Evaluation of Floating Microspheres of Sumatriptan Succinate using Ethyl Cellulose and Mucilage Extracted from Vigna Mungo

2021 ◽  
pp. 24-36
Author(s):  
Nilesh S. Kulkarni ◽  
Mukta A. Kulkarni ◽  
Rahul H. Khiste ◽  
Mohini C. Upadhye ◽  
Shashikant N. Dhole
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Polymer Concentration ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Vigna Mungo ◽  
Average Particle ◽  
Sumatriptan Succinate

Aim: The present investigation is to formulate and evaluate gastroretentive floating microspheres for sumatriptan succinate. Gastric retention is widely used approach to retain dosage form in stomach and to enhance absorption of drugs. Methods: The gastroretentive floating microspheres was prepared by two different techniques as solvent evaporation and W/O/W multiple emulsion technique. Ethyl cellulose, HPMC K4M polymer and mucilage extracted from Vigna Mungo in various proportions were used for formulation of microspheres. Combination of ethyl acetate and acetone in different proportion was used as organic phase and the microspheres were characterized for particle size, shape, morphology, percentage yield, entrapment efficiency, drug loading, In-Vitro Floating/Buoyancy study, In-vitro Floating/Buoyancy study and release kinetics. Results: The average particle size of all batches was found in the range 100 to 210 μm and the entrapment efficiency of all formulations was found in the range of 17.46 % to 59.28 %.Total floating time for Sumatriptan succinate floating microspheres was observed more than 12 h. The In-Vitro drug release study was performed for all formulations showed drug release in controlled manner. Conclusion: The particle size was increased with increased polymer concentration and it showed that polymer concentration has an impact on the entrapment efficiency. Ethyl cellulose microspheres showed more entrapment and sustained delivery of sumatriptan Succinate than microspheres prepared by combination of Ethyl cellulose: HPMC K4M and Ethyl cellulose: Vigna mungo mucilage.

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

2017 ◽  
Vol 9 (4) ◽  
pp. 54 ◽  
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. 

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

2018 ◽  
Vol 11 (5) ◽  
pp. 355 ◽  
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.

Naturally Derived Matrix for Controlled Selenium Nanoparticles Delivery

2016 ◽  
Vol 695 ◽  
pp. 284-288 ◽  
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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