scholarly journals Synthesis and characterization of peptide conjugated human serum albumin nanoparticles for targeted cardiac uptake and drug delivery.

2021 ◽  
Author(s):  
Satya Prakash ◽  
Nikita Lomis ◽  
Susan Westfall ◽  
Dominique Shum-Tim
Keyword(s):  
Heart Failure ◽  
Drug Delivery ◽  
Human Serum Albumin ◽  
Serum Albumin ◽  
Human Serum ◽  
Targeted Delivery ◽  
H9c2 Cells ◽  
Albumin Nanoparticles ◽  
Body Retention

Congestive heart failure, a prominent cardiovascular disease results primarily from myocardial infarction or ischemia. Milrinone (MRN), a widely used clinical drug for heart failure, improves myocardial contractility and cardiac function through its inotropic and vasodilatory effects. However, lacking target specificty, it exhibits low bioavailability and lower body retention time. Therefore, in this study, angiotensin II (AT1) peptide conjugated human serum albumin nanoparticles (AT1-HSA-MRN-NPs) have been synthesized for targeted delivery of MRN to the myocardium, overexpressing AT1 receptors under heart failure. The NPs were surface functionalized through a covalent conjugation reaction between HSA and AT1. Nanoparticle size was 215.2±4.7 nm and zeta potential -28.8±2.7 mV and cumulative release of MRN was ~72% over 24 hrs. The intracellular uptake of nanoparticles and cell viability was studied in H9c2 cells treated with AT1-MRN-HSA-NPs vs the control non-targeted drug, MRN Lactate under normal, hypoxic and hypertrophic conditions. The uptake of AT1-HSA-MRN-NPs in H9c2 cells was significantly higher as compared to non-targeted nanoparticles, and the viability of H9c2 cells treated with AT1-MRN-HSA-NPs vs MRN Lactate was 73.4±1.4% vs 44.9±1.4%, respectively. Therefore, AT1-HSA-MRN-NPs are safe for in vivo use and exhibit superior targeting and drug delivery characteristics for treatment of heart failure.

scholarly journals Synthesis and characterization of peptide conjugated human serum albumin nanoparticles for targeted cardiac uptake and drug delivery

PLoS ONE ◽  
2021 ◽  
Vol 16 (9) ◽  
pp. e0254305
Author(s):  
Nikita Lomis ◽  
Susan Westfall ◽  
Dominique Shum-Tim ◽  
Satya Prakash
Keyword(s):  
Heart Failure ◽  
Drug Delivery ◽  
Human Serum Albumin ◽  
Serum Albumin ◽  
Human Serum ◽  
Targeted Delivery ◽  
H9c2 Cells ◽  
Albumin Nanoparticles ◽  
Body Retention

Congestive heart failure, a prominent cardiovascular disease results primarily from myocardial infarction or ischemia. Milrinone (MRN), a widely used clinical drug for heart failure, improves myocardial contractility and cardiac function through its inotropic and vasodilatory effects. However, lacking target specificity, it exhibits low bioavailability and lower body retention time. Therefore, in this study, angiotensin II (AT1) peptide conjugated human serum albumin nanoparticles (AT1-HSA-MRN-NPs) have been synthesized for targeted delivery of MRN to the myocardium, overexpressing AT1 receptors under heart failure. The NPs were surface functionalized through a covalent conjugation reaction between HSA and AT1. Nanoparticle size was 215.2±4.7 nm and zeta potential -28.8±2.7 mV and cumulative release of MRN was ~72% over 24 hrs. The intracellular uptake of nanoparticles and cell viability was studied in H9c2 cells treated with AT1-MRN-HSA-NPs vs the control non-targeted drug, MRN Lactate under normal, hypoxic and hypertrophic conditions. The uptake of AT1-HSA-MRN-NPs in H9c2 cells was significantly higher as compared to non-targeted nanoparticles, and the viability of H9c2 cells treated with AT1-MRN-HSA-NPs vs MRN Lactate was 73.4±1.4% vs 44.9±1.4%, respectively. Therefore, AT1-HSA-MRN-NPs are safe for in vivo use and exhibit superior targeting and drug delivery characteristics for treatment of heart failure.

The in vivo antitumor activity of LHRH targeted methotrexate–human serum albumin nanoparticles in 4T1 tumor-bearing Balb/c mice

2012 ◽  
Vol 431 (1-2) ◽  
pp. 183-189 ◽  
Author(s):  
Azade Taheri ◽  
Rassoul Dinarvand ◽  
Fatemeh Ahadi ◽  
Mohammad Reza Khorramizadeh ◽  
Fatemeh Atyabi
Keyword(s):  
Human Serum Albumin ◽  
Antitumor Activity ◽  
Serum Albumin ◽  
Human Serum ◽  
Albumin Nanoparticles ◽  
Tumor Bearing ◽  
In Vivo Antitumor Activity

Preparation and formulation optimization of methotrexate-loaded human serum albumin nanoparticles modified by mannose

2021 ◽  
Vol 28 ◽  
Author(s):  
Zhenyu Chen ◽  
Zhongling Luo ◽  
Jiayao Lyu ◽  
Jianxin Wang ◽  
Zhongbing Liu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Human Serum Albumin ◽  
Serum Albumin ◽  
Human Serum ◽  
Drug Delivery System ◽  
Delivery System ◽  
Circulation Time ◽  
Independent Variables ◽  
Albumin Nanoparticles

Background: Methotrexate (MTX) is the representative drug among the disease-modifying anti-rheumatic drugs. But the conventional treatment with MTX showed many limitations and side effects. Objective: To strengthen the targeting ability and circulation time of MTX in the treatment of rheumatoid arthritis, the present study focused on developing a novel drug delivery system of methotrexate-loaded human serum albumin nanoparticles (MTX-NPs) modified by mannose, which referred as MTX-M-NPs. Methods: Firstly, mannose-derived carboxylic acid was synthesized and further modified on the surface of MTX-NPs to prepare MTX-M-NPs. The formulation of nanoparticles was optimized by method of central composite design (CCD), with the drug lipid ratio, oil-aqueous ratio, and cholesterol or lecithin weight as the independent variables. The average particle size and encapsulation efficiency were the response variables. Response of different formulations was calculated and the response surface diagram, contour diagram and mathematical equation were used to relate the dependent and independent variables to predict the optimal formula ratio. The uptake of MTX-M-NPs by neutrophils was studied through the laser confocal detection. Further, MTX-M-NPs was subjected to assess the pharmacokinetics profile after intravenous injection with Sprague-Dawley rats. Results: This targeting drug delivery system was successfully developed. Results from Nuclear Magnetic Resonance and Fourier Transform Infrared Spectroscopy analysis can verify the successful preparation of this drug delivery system. Based on the optimized formula, MTX-M-NPs was prepared with a particle size of 188.17 ± 1.71 nm and an encapsulation rate of 95.55 ± 0.33%. MTX-M-NPs displayed significantly higher cellular uptake than MTX-NPs. The pharmacokinetic results showed that MTX-M-NPs could prolong the in vivo circulation time of MTX. Conclusion: This targeting drug delivery system laid a promising foundation for the treatment of RA.

scholarly journals FABRICATION AND EVALUATION OF HUMAN SERUM ALBUMIN (HSA) NANOPARTICLES FOR DRUG DELIVERY APPLICATION

2009 ◽  
Vol 08 (03) ◽  
pp. 319-322 ◽  
Author(s):  
R. MEHRAVAR ◽  
M. JAHANSHAHI ◽  
N. SAGHATOLESLAMI
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Human Serum Albumin ◽  
Serum Albumin ◽  
Human Serum ◽  
Ph Value ◽  
Drug Carrier ◽  
Particle Size Analyzer ◽  
Carrier Systems

Human Serum Albumin (HSA) nanoparticles represent promising drug carrier systems. Particle size is a crucial parameter in particular for the in vivo behavior of nanoparticles after intravenous injection. The object of present study was to characterize the desolvation process of HSA for preparation of nanoparticles. Two process parameters were examined to achieve a suitable size of nanoparticles such as the pH value and the amount of glutaraldehyde concentration (%). The smallest size of nanoparticles achieved was 91 nm and the largest size was 388 nm which is suitable for drug delivery. The pH value of the HSA solution prior to the desolvation procedure was identified as the major factor determining particle size and the amount of crosslinker showed that it has less effect on produced nanoparticle size. The nanoparticle sample was purified by five cycles' centrifugation (20 000× g, 8 min) and redispersion of the pellet to the original volume in 10 mM NaCl at pH values of 7.5–9, respectively, and then analyzed by particle size analyzer (PCS).

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