Inhibition of serum angiotensin-converting enzyme in rabbits after intravenous administration of enalaprilat-loaded intact erythrocytes

Hamidi, Mehrdad; Tajerzadeh, Hosnieh; Dehpour, Ahmad‐Reza; Ejtemaee-Mehr, Shahram

doi:10.1111/j.2042-7158.2001.tb01796.x

Cited by 13 publications

(8 citation statements)

References 19 publications

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“…While in plasma it reaches only 72% after 23 hours. These results are comparable to results reported on similar polar drugs including gentamicin38, enalaprilat 39 and heparin 40. Hemoglobin release kinetics is belonged to zero order pattern while pravastatin is belonged to first order kinetics in both two phases.…”

Section: Resultssupporting

confidence: 87%

Characterization of Human Erythrocytes as Potential Carrier for Pravastatin: An In Vitro Study

Harisa¹,

Ibrahim²,

Alanazi³

2011

Int. J. Med. Sci.

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Drug delivery systems including chemical, physical and biological agents that enhance the bioavailability, improve pharmacokinetics and reduce toxicities of the drugs. Carrier erythrocytes are one of the most promising biological drug delivery systems investigated in recent decades. The bioavailability of statin drugs is low due the effects of P-glycoprotein in the gastro-intestinal tract as well as the first-pass metabolism. Therefore in this work we study the effect of time, temperature as well as concentration on the loading of pravastatin in human erythrocytes to be using them as systemic sustained release delivery system for this drug. After the loading process is performed the carriers' erythrocytes were physically and cellulary characterized. Also, the in vitro release of pravastatin from carrier erythrocytes was studied over time interval. Our results revealed that, human erythrocytes have been successfully loaded with pravastatin using endocytosis method either at 25oC or at 37oC. The loaded amount at 10 mg/ml is 0.32mg/0.1 ml and 0.69 mg/0.1 ml. Entrapment efficiency is 34% and 94% at 25oC and 37oC respectively at drug concentration 4 mg/ml. Moreover the percent of cells recovery is 87-93%. Hematological parameters and osmotic fragility behavior of pravastatin loaded erythrocytes were similar that of native erythrocytes. Scanning electron microscopy demonstrated that the pravastatin loaded cells has no change in the morphology. Pravastatin releasing from carrier cell was 83% after 23 hours in phosphate buffer saline and decreased to 72% by treatment of carrier cells with glutaraldehyde. The releasing pattern of the drug from loaded erythrocytes obeyed first order kinetics. It concluded that pravastatin is successfully entrapped into erythrocytes with acceptable loading parameters and moderate morphological changes, this suggesting that erythrocytes can be used as prolonged release for pravastatin.

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Section: Resultssupporting

confidence: 87%

Characterization of Human Erythrocytes as Potential Carrier for Pravastatin: An In Vitro Study

Harisa¹,

Ibrahim²,

Alanazi³

2011

Int. J. Med. Sci.

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“…Several studies reported the effect of drugs on fragility behavior of erythrocytes. Hamidi and his workers stated that osmotic fragility of loaded erythrocytes is lower than unloaded cells 23 . On contrast, another study revealed that osmotic fragility of carrier erythrocytes is higher than unloaded cells 24 .…”

Section: Osmotic Fragility Behavior Of Salbutamol Loaded Erythrocytesmentioning

confidence: 99%

Preparation and In Vitro Evaluation of Resealed Erythrocytes as A New Trend in Treatment of Asthma

Ibrahim

Zaky

Afouna

et al. 2016

IJDDT

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Carrier erythrocytes are emerging as one of the most promising biological drug delivery systems investigated in recent decades. Beside its biocompatibility, biodegradability and ability to circulate throughout the body, it has the ability to perform extended release system of the drug for a long period. The ultimate goal of this study is to introduce a new carrier system for Salbutamol, maintaining suitable blood levels for a long time, as atrial to resolve the problems of nocturnal asthma medication Therefore in this work we study the effect of time, temperature as well as concentration on the loading of salbutamol in human erythrocytes to be used as systemic sustained release delivery system for this drug. After the loading process is performed the carrier erythrocytes were physically and cellulary characterized. Also, the in vitro release of salbutamol from carrier erythrocytes was studied over time interval. From the results it was found that, human erythrocytes have been successfully loaded with salbutamol using endocytosis method either at 25 Co or at 37 Co . The highest loaded amount was 3.5 mg/ml and 6.5 mg/ml respectively. Moreover, the percent of cells recovery is 90.7± 1.64%. Hematological parameters and osmotic fragility behavior of salbutamol loaded erythrocytes were similar that of native erythrocytes. Scanning electron microscopy demonstrated that the salbutamol loaded cells has moderate change in the morphology. Salbutamol releasing from carrier cell was 43% after 36 hours in phosphate buffer saline. The releasing pattern of the drug from loaded erythrocytes showed initial burst release in the first hour followed by a very slow release, obeying zero order kinetics. It concluded that salbutamol is successfully entrapped into erythrocytes with acceptable loading parameters and moderate morphological changes, this suggesting that erythrocytes can be used as prolonged release carrier for salbutamol.

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“…As an advantage, in the optimum conditions of the loading procedure (using more gentle methods for loading), the life‐span of the resulting carrier cells may be comparable with that of normal erythrocytes [1,6,7] . Erythrocytes have been used as circulating intravenous slow‐release carriers for the delivery of antineoplasm agents, antiparasitic drugs, antiretroviral agents, vitamins, steroids, antibiotics, and cardiovascular drugs among others [1,6–34] …”

Section: Introductionmentioning

confidence: 99%

Preparation and in-vitro characterization of tramadol-loaded carrier erythrocytes for long-term intravenous delivery

Foroozesh

Hamidi

Zarrin

et al. 2011

Journal of Pharmacy and Pharmacology

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Inhibition of serum angiotensin-converting enzyme in rabbits after intravenous administration of enalaprilat-loaded intact erythrocytes

Cited by 13 publications

References 19 publications

Characterization of Human Erythrocytes as Potential Carrier for Pravastatin: An In Vitro Study

Characterization of Human Erythrocytes as Potential Carrier for Pravastatin: An In Vitro Study

Preparation and In Vitro Evaluation of Resealed Erythrocytes as A New Trend in Treatment of Asthma

Preparation and in-vitro characterization of tramadol-loaded carrier erythrocytes for long-term intravenous delivery

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