Design and Charecterization of Anticancer Engineered Resealed Erythrocytes

1970 ◽  
Vol 1 (3) ◽  
pp. 243-250
Author(s):  
R. C. Doijad ◽  
N. V. Deshmukh ◽  
D. S. Bhambere ◽  
Rony Joseph ◽  
F. V. Manvi
Keyword(s):  
Targeted Delivery ◽  
Release Kinetics ◽  
Reticuloendothelial System ◽  
Sem Analysis ◽  
In Vitro Tests ◽  
Mean Corpuscular Hemoglobin ◽  
Laser Scattering ◽  
Zero Order Kinetics ◽  
Model Drug

A number of investigators have been focusing their attention on the encapsulation of antineoplastic drugs within erythrocytes to diminish their side effects. In this study, human erythrocytes have been loaded by methotrexate (MTX) as a model drug using hypotonic hemolysis method for targeted delivery of this drug. A series of in vitro tests have been carried out to characterize the carrier cells in vitro, including loading parameters, hemoglobin release kinetics, particle size distribution, SEM analysis, osmotic and turbulence fragilities. Carrier erythrocytes having acceptable loading parameters, released their drug content according to zero-order kinetics. Mean corpuscular hemoglobin content values of the cells decreased, the apparent cell sizes measured using dynamic laser scattering, were not significantly different from normal erythrocytes, but the real sizes, measured using SEM, and surface topologies were quite different between loaded and unloaded cells. The MTX-loaded cells were remarkably more fragile compared to the normal cells. Drug loaded erythrocytes showed preferential drug targeting to liver followed by lungs, kidney and spleen. Totally, MTX-loaded erythrocytes seem to be a promising delivery system for targeting the drug to reticuloendothelial system (RES).

scholarly journals Double-Walled Poly-(D,L-lactide-co-glycolide) (PLGA) and Poly(L-lactide) (PLLA) Nanoparticles for the Sustained Release of Doxorubicin

Polymers ◽  
2021 ◽  
Vol 13 (19) ◽  
pp. 3230
Author(s):  
M. Margarida Cardoso ◽  
Inês N. Peca ◽  
Telma Lopes ◽  
Rui Gardner ◽  
A. Bicho
Keyword(s):  
Rate Control ◽  
Release Kinetics ◽  
Drug Distribution ◽  
In Vitro Tests ◽  
Cellular Viability ◽  
Release Rates ◽  
Zero Order Release ◽  
Evaporation Technique ◽  
Model Drug

Double-walled nanoparticles (DWNPs), containing doxorubicin as a model drug, were produced using poly-(D,L-lactide-co-glycolide) (PLGA) and poly(L-lactide) (PLLA) by the solvent evaporation technique. Double-walled microparticles containing doxorubicin were also produced to make possible the examination of the inner morphology and drug distribution using optical and fluorescence microscopy. The produced microparticles present a double-walled structure with doxorubicin solubilized in the PLGA-rich phase. The DWNPs produced present very low initial burst values and a sustained DOX release for at least 90 days with release rates decreasing with the increase in the PLLA amount. Zero-order release kinetics were obtained after day 15. The results support that the PLLA layer acts as a rate control barrier and that the diffusion of doxorubicin from the drug-loaded inner PLGA core can be retarded by an increase in the thickness of the unloaded outer layer. The unloaded double-walled nanoparticles produced were used in in vitro tests with CHO cells and demonstrate that they are nontoxic, while the double-walled nanoparticles loaded with doxorubicin caused a great cellular viability and decreased when tested in vitro.

3 (2) Factorial Design Assisted Crushed Puffed Rice-HPMC-Chitosan based Hydrodynamically Balanced System of Metoprolol Succinate

2020 ◽  
Vol 10 (3) ◽  
pp. 237-249
Author(s):  
Shashank Soni ◽  
Veerma Ram ◽  
Anurag Verma
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Hydroxypropyl Methylcellulose ◽  
Batch Size ◽  
Metoprolol Succinate ◽  
Zero Order Kinetics ◽  
Two Factors ◽  
Puffed Rice ◽  
Model Drug

Introduction: Hydrodynamically balanced system (HBS) possesses prolonged and continuous delivery of the drug to the gastrointestinal tract which improves the rate and extent of medications that have a narrow absorption window. The objective of this work was to develop a Hydrodynamically Balanced System (HBS) of Metoprolol Succinate (MS) as a model drug for sustained stomach specific delivery. Materials and Methods: Experimental batches were designed according to 3(2) Taguchi factorial design. A total of 9 batches were prepared for batch size 100 capsules each. Formulations were prepared by physically blending MS with polymers followed by encapsulation into hard gelatin capsule shell of size 0. Polymers used were Low Molecular Weight Chitosan (LMWCH), Crushed Puffed Rice (CPR), and Hydroxypropyl Methylcellulose K15 M (HPMC K15M). Two factors used were buoyancy time (Y1) and time taken for 60% drug release (T60%; Y2). Results: The drug excipient interaction studies were performed by the thermal analysis method which depicts that no drug excipient interaction occurs. In vitro buoyancy studies and drug release studies revealed the efficacy of HBS to remain gastro retentive for a prolonged period and concurrently sustained the release of MS in highly acidic medium. All formulations followed zero-order kinetics. Conclusion: Developed HBS of MS with hydrogel-forming polymers could be an ideal delivery system for sustained stomach specific delivery and would be useful for the cardiac patients where the prolonged therapeutic action is required.

scholarly journals Development of a reservoir type prolonged release system with felodipine via simplex methodology

2015 ◽  
Vol 89 (1) ◽  
pp. 128-136
Author(s):  
Rareș Iuliu Iovanov ◽  
Ioan Tomuță ◽  
Sorin Emilian Leucuța
Keyword(s):  
Simplex Method ◽  
Release Kinetics ◽  
Prolonged Release ◽  
Lauryl Sulfate ◽  
Pore Former ◽  
Release System ◽  
Reservoir Type ◽  
Model Drug ◽  
Kinetics Of

Background and aims. Felodipine is a dihydropyridine calcium antagonist that presents good characteristics to be formulated as prolonged release preparations. The aim of the study was the formulation and in vitro characterization of a reservoir type prolonged release system with felodipine, over a 12 hours period using the Simplex method.Methods. The first step of the Simplex method was to study the influence of the granules coating method on the felodipine release. Furthermore the influence of the coating polymer type, the percent of the coating polymer and the percent of pore forming agent in the coating on the felodipine release were studied. Afterwards these two steps of the experimental design the percent of Surelease applied on the felodipine loaded granules and the percent of pore former in the polymeric coating formulation variables were studied. The in vitro dissolution of model drug was performed in phosphate buffer solution (pH 6.5) with 1% sodium lauryl sulfate. The released drug quantification was done using an HPLC method. The release kinetics of felodipine from the final granules was assessed using different mathematical models.Results. A 12 hours release was achieved using granules with the size between 315 – 500 µm coated with 45% Surelease with different pore former ratios in the coating via the top-spray method.Conclusion. We have prepared prolonged release coated granules with felodipine using a fluid bed system based on the Simplex method. The API from the studied final formulations was released over a 12 hours period and the release kinetics of the model drug substance from the optimized preparations fitted best the Higuchi and Peppas kinetic models. 

scholarly journals Formulation Development and Evaluation of Drug Release Kinetics from Colon-Targeted Ibuprofen Tablets Based on Eudragit RL 100-Chitosan Interpolyelectrolyte Complexes

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Kenneth Chibuzor Ofokansi ◽  
Franklin Chimaobi Kenechukwu
Keyword(s):  
Drug Release ◽  
Targeted Delivery ◽  
Release Kinetics ◽  
Local Treatment ◽  
Wet Granulation ◽  
Formulation Development ◽  
Swelling Properties ◽  
Interpolyelectrolyte Complexes ◽  
Bowel Diseases

Colon-targeted drug delivery systems (CTDDSs) could be useful for local treatment of inflammatory bowel diseases (IBDs). In this study, various interpolyelectrolyte complexes (IPECs), formed between Eudragit RL100 (EL) and chitosan (CS), by nonstoichiometric method, and tablets based on the IPECs, prepared by wet granulation, were evaluated as potential oral CTDDSs for ibuprofen (IBF). Results obtained showed that the tablets conformed to compendial requirements for acceptance and that CS and EL formed IPECs that showed pH-dependent swelling properties and prolonged the in vitro release of IBF from the tablets in the following descending order: 3 : 2 > 2 : 3 > 1 : 1 ratios of CS and EL. An electrostatic interaction between the carbonyl (–CO–) group of EL and amino (–) group of CS of the tablets formulated with the IPECs was capable of preventing drug release in the stomach and small intestine and helped in delivering the drug to the colon. Kinetic analysis of drug release profiles showed that the systems predominantly released IBF in a zero-order manner. IPECs based on CS and EL could be exploited successfully for colon-targeted delivery of IBF in the treatment of IBDs.

Anaphylactic Shock following Povidone

1996 ◽  
Vol 30 (1) ◽  
pp. 37-40 ◽  
Author(s):  
Ma Angeles Gonzalo Garijo ◽  
José A Durán Quintana ◽  
Pedro Bobadilla González ◽  
Pilar Máiquez Asuero
Keyword(s):  
Anaphylactic Reaction ◽  
Benzalkonium Chloride ◽  
Reticuloendothelial System ◽  
Pharmaceutical Products ◽  
In Vitro Tests ◽  
Polysorbate 80 ◽  
Provocation Tests ◽  
Release Histamine ◽  
Intraarticular Administration

OBJECTIVE: To report a patient with an anaphylactic reaction related to povidone administration. CASE SUMMARY: A 37-year-old man with a history of allergic rhinitis presented with urticaria, dyspnea, wheezing, rhinorrhea, and dysphonia 20 minutes after the intraarticular administration of mepivacaine hydrochloride and paramethasone acetate in his right knee. Two months after this episode, he was admitted for controlled provocation tests. Tests on mepivacaine were negative. The preparation of paramethasone contained the excipients benzalkonium chloride, polysorbate 80, and povidone. In vitro tests and provocation were negative with polysorbate 80 and benzalkonium chloride, but positive with povidone. DISCUSSION: Povidone, a mixture of synthetic polymers, is commonly used as an excipient in pharmaceutical products, an additive in food products, and a dispersant and stabilizer in hairsprays. Although it is well tolerated when used topically or parenterally, local and systemic effects have been reported. Furthermore, multiorgan involvement resulting from accumulation of the drug in the reticuloendothelial system has been described. The immunologic properties of povidone have not been explored in humans, but have been in animals. In fact, the capacity of povidone to release histamine and its immunogenicity are proportional to its molecular weight. An immunoglobulin (Ig) E-mediated hypersensitivity reaction in asthma has been reported. In our case, povidone was responsible for the syndrome. However, we cannot determine the exact mechanism. An unspecific histamine release and/or an IgE-mediated hypersensitivity could be involved. CONCLUSIONS: Povidone was responsible for a severe anaphylactic reaction in our patient. The possibility of an iatrogenic adverse effect caused by the excipient but not by the active ingredient should be considered in patients exhibiting similar symptoms. We believe that the excipients used in the preparation of all medicines should be disclosed.

Controlled Release of Bone Growth Factors from Injectable, Biodegradable Polymer Scaffolds for Bone Tissue Engineering

2000 ◽  
Vol 662 ◽  
Author(s):  
Elizabeth L. Hedberg ◽  
Antonios G. Mikos
Keyword(s):  
Growth Factors ◽  
Controlled Release ◽  
Bone Growth ◽  
Bone Ingrowth ◽  
Release Kinetics ◽  
Salt Content ◽  
Burst Effect ◽  
Plga Microparticles ◽  
Model Drug

AbstractThe objective of this research is to fabricate injectable, polymeric composites that will act as scaffolds for bone ingrowth as well as carriers for the controlled release of bone growth factors. To that end, the injectable polyester poly(propylene fumarate) (PPF) was loaded with poly(DLlactic-co-glycolic acid) (PLGA) microparticles carrying the model drug FITC-dextran. This preparation was then crosslinked with N-vinyl pyrrolidinone in the presence of benzoyl peroxide as initiator and sodium chloride (NaCl) as leachable porogen. The encapsulation of growth factors in microparticles is necessary to minimize their denaturation during scaffold crosslinking. PLGA microparticles (0.04 g microparticles/g PPF) were incorporated into PPF composites having variable NaCl weight percents (50 and 70 wt% NaCl) and the effect on FITC-dextran release kinetics was determined in vitro for cylinders of diameter 6.5 mm and height 13.0 mm. The FITC-dextran loaded microparticles alone exhibited a large initial burst effect, while the composite materials displayed a smaller burst effect and a longer linear region of release. At day 3, 54.6±2.1%, 5.1±0.9%, and 12.5±0.3% of loaded FITC-dextran was released into pH 7.4 phosphate buffered saline from the microparticles, the 50 wt% NaCl, and the 70 wt% NaCl composites, respectively. By day 28, 90.9±6.9%, 12.7±1.7%, and 34.4±0.4% of loaded FITC-dextran was released. Our results demonstrate that PLGA microparticles can be incorporated into PPF composites and that the release kinetics of FITC-dextran can be systematically manipulated through alteration of the composite initial salt content.

10 IN VITRO PROGESTERONE RELEASE KINETICS: A COMPARATIVE STUDY OF DIFFERENT INTRAVAGINAL DEVICES USED IN CATTLE

2011 ◽  
Vol 23 (1) ◽  
pp. 111
Author(s):  
G. C. Gomes ◽  
A. Kehrle ◽  
M. Maturana Filho ◽  
C. V. F. Caetano ◽  
J. R. V. Pimentel ◽  
...  
Keyword(s):  
Statistical Difference ◽  
Release Kinetics ◽  
In Vitro Tests ◽  
Water Mixture ◽  
The Third ◽  
Metabolism Rate ◽  
Alcohol Water ◽  
Reproduction Cost ◽  
Second Use

Since progesterone releasing devices have been used for oestrous cycle control, many studies have been done to evaluate the reduce reproduction cost. However, there are few studies about reused devices. The aim of this study was to evaluate and compare in vitro P4 releasing kinetics from 3 commercially available devices: Sincrogest® (SIN, 1 g of P4), Cronipres® (CRO, 1 g of P4 and 3 rings of 0.1 g of P4 for the third use), and Primer® (PRI, 1 g of P4). For each device, new (first use, n = 2), once-used (second use, n = 2), and twice-used (third use, n = 2) devices were tested. The tests were performed in a dissolutor sink using an alcohol/water mixture (60/40, vol/vol) as a release media. Samples were collected at 0–24 h (1P), 24–48 h (2P), 48–72 h (3P), and 72–96 h (4P). Table 1 shows the P4 amount (mg) and standard deviation in the periods in which there was statistical difference (P < 0.05; a–cdifferent letters in the same period differ statistically). The 3 brands of P4 devices differ in 2 of 4, 3 of 4, and 1 of 4 intervals for 1st-, 2nd, and 3rd-use device tests respectively. Additionally, P4 release decreased according to the number of previous uses. It is known that in vitro tests are more sensible to detect differences between devices. Nevertheless, these findings suggest the possibility of targeting different device categories for different animal categories depending on the animal steroid metabolism rate and consequent need for exogenous P4. However, for such a claim, further studies on this topic are needed. Table 1.Comparison between the 3 types in each of 3 uses Supported by FAPESP – Fundação de Amparo a Pesquisa do estado de São Paulo.

scholarly journals Drug Release Kinetics of Electrospun PHB Meshes

Materials ◽  
2019 ◽  
Vol 12 (12) ◽  
pp. 1924 ◽  
Author(s):  
Vojtech Kundrat ◽  
Nicole Cernekova ◽  
Adriana Kovalcik ◽  
Vojtech Enev ◽  
Ivana Marova
Keyword(s):  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Toxic Substances ◽  
Antimicrobial Efficiency ◽  
Vis Spectroscopy ◽  
Model Drug ◽  
Phosphate Buffered Saline ◽  
Kinetics Of

Microbial poly(3-hydroxybutyrate) (PHB) has several advantages including its biocompatibility and ability to degrade in vivo and in vitro without toxic substances. This paper investigates the feasibility of electrospun PHB meshes serving as drug delivery systems. The morphology of the electrospun samples was modified by varying the concentration of PHB in solution and the solvent composition. Scanning electron microscopy of the electrospun PHB scaffolds revealed the formation of different morphologies including porous, filamentous/beaded and fiber structures. Levofloxacin was used as the model drug for incorporation into PHB electrospun meshes. The entrapment efficiency was found to be dependent on the viscosity of the PHB solution used for electrospinning and ranged from 14.4–81.8%. The incorporation of levofloxacin in electrospun meshes was confirmed by Fourier-transform infrared spectroscopy and UV-VIS spectroscopy. The effect of the morphology of the electrospun meshes on the levofloxacin release profile was screened in vitro in phosphate-buffered saline solution. Depending upon the morphology, the electrospun meshes released about 14–20% of levofloxacin during the first 24 h. The percentage of drug released after 13 days increased up to 32.4% and was similar for all tested morphologies. The antimicrobial efficiency of all tested samples independent of the morphology, was confirmed by agar diffusion testing.

scholarly journals The Removal of in Vitro Damaged Erythrocytes from the Circulation of Normal and Splenectomized Rats

Blood ◽  
1965 ◽  
Vol 26 (1) ◽  
pp. 49-62 ◽  
Author(s):  
JOHN E. ULTMANN ◽  
CLARA S. GORDON
Keyword(s):  
Life Span ◽  
Osmotic Fragility ◽  
Reticuloendothelial System ◽  
Red Cells ◽  
In Vitro Tests ◽  
Red Cell ◽  
Cell Integrity ◽  
Prolonged Incubation

Abstract The in vitro alterations and in vivo fate of erythrocytes treated with N-ethylmaleimide or subjected to prolonged incubation were studied in normal and splenectomized rats. Minimal injury (20 µM NEM/ml. RBC) resulted in red cells with decreased osmotic fragility and increased plasticity; however, mechanical fragility was significantly increased. These cells were removed with a half-time of 78 minutes, mainly by splenic sequestration, and splenectomy prolonged their life span. Incubation at 37 C. for 21 hours produced erythrocytes with increased osmotic and mechanical fragility and decreased plasticity. Erythrocyte clearance was more rapid (T½ = 59 minutes), with spleen and liver removing approximately an equal number of cells and splenectomy having little effect on red cell life span. With severe injury (40 µM NEM/ml. RBC), all three in vitro measurements showed marked alterations, red cell removal was rapid (T½ = 35 minutes), mainly by hepatic sequestration, and clearance was unaffected by splenectomy. The present studies have shown that chemical injury or prolonged incubation lead to profound changes in in vitro tests of red cell integrity, the mechanical fragility predicting most closely the subsequent in vivo events. Although the entire reticuloendothelial system appears to participate in red cell removal, the spleen and liver are the major sites of sequestration in the rat. The splenic removal predominates with minimally injured cells, hepatic removal with moderately and severely altered cells. The type of injury appears to be of less significance than the degree of injury of the red cells.

scholarly journals Preparation and in vitro release kinetics of nitrendipine-loaded PLLA–PEG–PLLA microparticles by supercritical solution impregnation process

RSC Advances ◽  
2019 ◽  
Vol 9 (28) ◽  
pp. 16167-16175 ◽  
Author(s):  
Shiping Zhan ◽  
Jingchang Wang ◽  
Weijing Wang ◽  
Liyun Cui ◽  
Qicheng Zhao
Keyword(s):  
Release Kinetics ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Impregnation Process ◽  
Supercritical Solution ◽  
Model Drug ◽  
Polymer Microparticles ◽  
Kinetics Of ◽  
Vitro Release

In this work, drug-loaded polymer microparticles were prepared by a supercritical solution impregnation (SSI) process with nitrendipine as the model drug and PLLA–PEG–PLLA as the drug carrier.

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