scholarly journals Rapamycin-Loaded Polymeric Nanoparticles as an Advanced Formulation for Macrophage Targeting in Atherosclerosis

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 503
Author(s):  
Emanuela Fabiola Craparo ◽  
Marta Cabibbo ◽  
Alice Conigliaro ◽  
Maria Magdalena Barreca ◽  
Teresa Musumeci ◽  
...  
Keyword(s):  
Polymeric Nanoparticles ◽  
Drug Loading ◽  
Mammalian Target Of Rapamycin ◽  
Amorphous State ◽  
Entrapment Efficiency ◽  
Polymeric Nanoparticle ◽  
Specific Accumulation ◽  
Cd36 Receptor

Recently, rapamycin (Rapa) represents a potential drug treatment to induce regression of atherosclerotic plaques; however, its use requires site-specific accumulation in the vessels involved in the formation of the plaques to avoid the systemic effects resulting from its indiscriminate biodistribution. In this work, a stable pharmaceutical formulation for Rapa was realized as a dried powder to be dispersed extemporaneously before administration. The latter was constituted by mannitol (Man) as an excipient and a Rapa-loaded polymeric nanoparticle carrier. These nanoparticles were obtained by nanoprecipitation and using as a starting polymeric material a polycaprolactone (PCL)/α,β-poly(N-2-hydroxyethyl)-dl-aspartamide (PHEA) graft copolymer. To obtain nanoparticles targeted to macrophages, an oxidized phospholipid with a high affinity for the CD36 receptor of macrophages, the 1-(palmitoyl)-2-(5-keto-6-octene-dioyl) phosphatidylcholine (KOdia-PC), was added to the starting organic phase. The chemical–physical and technological characterization of the obtained nanoparticles demonstrated that: both the drug loading (DL%) and the entrapment efficiency (EE%) entrapped drug are high; the entrapped drug is in the amorphous state, protected from degradation and slowly released from the polymeric matrix; and the KOdia-PC is on the nanoparticle surface (KP-Nano). The biological characterization demonstrated that both systems are quickly internalized by macrophages while maintaining the activity of the drug. In vitro studies demonstrated that the effect of KP-Nano Rapa-loaded, in reducing the amount of the Phospo-Ser757-ULK1 protein through the inhibition of the mammalian target of rapamycin (mTOR), is comparable to that of the free drug.

scholarly journals PREPARATION AND CHARACTERIZATION OF THYMOQUINONE NANOPARTICLES PEGYLATED AS DRUG DELIVERY SYSTEM

2021 ◽  
Author(s):  
A. Hasrawati ◽  
Irsan Rizaldi ◽  
Deisy Febrianti ◽  
A Mumtihanah Mursyid ◽  
Neneng Amelia Bakri
Keyword(s):  
Peer Review ◽  
Nigella Sativa ◽  
Drug Loading ◽  
Physicochemical Characterization ◽  
Entrapment Efficiency ◽  
Peg 6000 ◽  
Black Cumin ◽  
Main Component

Objective: Thymoquinone is a main component of Black Cumin (Nigella  sativa Linn.) with various pharmacological activities, but has poor stability and bioavailability. The purpose of this study was to carry out the preparation and characterization of timoquinone nanoparticles PEGylation. Methods: The Thymoquinone nanoparticles  (TQ-NP) were made with PEGylation using PEG 6000 with the concentrations on each preparation of 3 mM (A), 4 mM (B), and 5 mM (C) then were evaluated by the parameter of yield percentage Entrapment Efficiency (EE) and Drug Loading (DL), drug release, size and distribution particle, morphological analysis and Fourier Transform-Infrared spectrophotometer (FTIR). Results: Thymoquinone nanoparticle was PEGylated with PEG 6000  has the highest efficiency entrapment of 99.9718±0.029% in formula A, with the capacity of drug loading 0,66%. Formulation A release 99.9718±0.029% of Thymoquinone at 50 minutes. The morphological observations with Scanning Electron Microscope (SEM) showed spherical nanoparticles morphology.                           Peer Review History: Received 11 September  2020; Revised 5 Decembe; Accepted 3 January, Available online 15 January 2021 UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file:                           Comments of reviewer(s):         Average Peer review marks at initial stage: 6.0/10 Average Peer review marks at publication stage: 8.0/10 Reviewer(s) detail: Dr. Evren Alğin Yapar, Turkish Medicines and Medical Devices Agency, Turkiye, [email protected] Dr. Sally A. El-Zahaby, Pharos University in Alexandria, Egypt, [email protected] Similar Articles: ABACAVIR LOADED NANOPARTICLES: PREPARATION, PHYSICOCHEMICAL CHARACTERIZATION AND IN VITRO EVALUATION LONG CHAIN POLYMERIC CARBOHYDRATE DEPENDENT NANOCOMPOSITES IN TISSUE ENGINEERING EFFECT OF PEGYLATED EDGE ACTIVATOR ON SPAN 60 BASED- NANOVESICLES: COMPARISON BETWEEN MYRJ 52 AND MYRJ 59

scholarly journals Preparation, Optimization and In vitro Evaluation of Glipizide Nanoparticles Integrated with Eudragit RS-100

2019 ◽  
Vol 7 (1) ◽  
pp. 72-85 ◽  
Author(s):  
P. Saharan ◽  
K. Bahmani ◽  
S.P. Saharan
Keyword(s):  
Particle Size ◽  
Factorial Design ◽  
Drug Loading ◽  
Amorphous State ◽  
Entrapment Efficiency ◽  
Pharmaceutical Products ◽  
Dose Frequency ◽  
Release Formulation ◽  
Pharmaceutical Industries

Background: Solubility is an important criterion for drug efficacy, independent of the route of administration. It also poses a major challenge for pharmaceutical industries, which are developing new pharmaceutical products, since 40% of the active substances being identified are either insoluble or poorly soluble in aqueous media. Objective: The objective of this study was to develop nanoformulation of glipizide drugloaded nanoparticles providing controlled release formulation. Method: Nanoparticles were prepared by the solvent evaporation method. Eudragit RS100, a nonbiodegradable polymer with varying ratios was used for making the formulation. The effect of key formulation variables on the particle size and entrapment efficiency and drug loading of nanoparticles were studied by using factorial design. Results: DSC thermograms indicate that glipizide was dispersed in an amorphous state in the polymer. TEM study indicates that the nanoparticles were in spherical shape. The mean diameter was dependent on the presence of the amount of Eudragit RS100 and viscosity of the organic phase. The in vitro study showed that the cumulative drug release was from 69.52-81.44 % in 10 hrs at pH 6.8 in phosphate buffer respectively. Conclusion: Conclusion: The developed NPs could reduce dose frequency, decrease side effects, and improve patient compliance. Using factorial design, maximum entrapment efficiency with minimum particle size could be achieved with a few experiments.

Transferrin Modified Dioscin Loaded PEGylated Liposomes: Characterization and In Vitro Antitumor Effect

2020 ◽  
Vol 20 (3) ◽  
pp. 1321-1331 ◽  
Author(s):  
Yuanyuan Wang ◽  
Yining Yang ◽  
Yibin Yu ◽  
Jinyu Li ◽  
Weisan Pan ◽  
...  
Keyword(s):  
Laser Scanning ◽  
Drug Loading ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Laser Scanning Confocal Microscopy ◽  
Average Particle ◽  
Scanning Confocal Microscopy ◽  
Drug Entrapment Efficiency

In this study, a novel transferrin modified liposomal dioscin was prepared by the film dispersion method. The transferrin modified dioscin loaded liposomes (Tf-Lip/Dio) were near-spherical in morphology and had an average particle size of 140.07±1.33 nm, a narrow polydispersity index of <0.2 and a relatively stable zeta potential of -23.7±1.16 mV. The drug entrapment efficiency (EE) and drug loading (DL) of Tf-Lip/Dio were 88.94±1.02% and 4.16±0.05%, respectively. Tf-Lip/Dio exhibited a sustained release characterization of approximately 30% of the total dioscin content after 72 h at 37 °C. Tf-Lip/Dio showed higher cytotoxic efficacy after incubation for 24 h in both HeLa cells and HepG2 cells than in nonmodified liposomes. The enhanced antitumor activity of Tf-Lip/Dio might be due to the increased intracellular uptake, which was corroborated by laser scanning confocal microscopy and flow cytometry. Furthermore, hemolysis experiments preliminarily verified the safety of its intravenous injection. Overall, this study demonstrates Tf-Lip/Dio to be a favorable delivery vehicle for dioscin in future cancer therapy.

Formulation, optimization, and characterization of amlodipine besylate loaded polymeric nanoparticles

2021 ◽  
Vol 29 (9_suppl) ◽  
pp. S1555-S1568
Author(s):  
Vibha Chourasiya ◽  
Sarvesh Bohrey ◽  
Archna Pandey
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Polymeric Nanoparticles ◽  
Entrapment Efficiency ◽  
Amlodipine Besylate ◽  
Process Yield ◽  
In Vitro Drug Release ◽  
Drug Entrapment Efficiency

The objectives of this work were to formulate and optimize amlodipine besylate loaded polymeric nanoparticles by using factorial design. The emulsion solvent evaporation method was employed successfully to produce the drug loaded polymeric nanoparticles and the optimization was done by the help of the 24 factorial design. The effect of the main preparation variables on the dependent variables such as nanoparticle size and % drug entrapment efficiency was studied for the optimization of the nanoparticles. The characterization of these nanoparticles was done by the different parameters such as interaction between the excipients, size, morphology, zeta potential, % drug entrapment efficiency, % process yield, and in-vitro drug release behavior. FTIR, DLS, TEM, AFM, zeta potential studies, and dialysis bag method were performed for this purpose. The in vitro drug release data were analyzed by different kinetic models to know the release mechanism. The optimized nanoparticles were spherical in shape and showed particle size 91.5 ± 4.3 nm, PDI 0.368 ± 0.014, zeta potential −17.5 mV, % drug entrapment efficiency 74.06 ± 2.1%, and % process yield 78.51 ± 1.8%. The release kinetics studies revealed that drug release from the nanoparticles follow the Korsmeyer–Peppas model.

FORMULATION AND CHARACTERIZATION OF RITONAVIR LOADED PRONIOSOMES FOR ORAL DRUG DELIVERY

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (08) ◽  
pp. 46-53
Author(s):  
T. A Sande ◽  
◽  
F. J Sayyad ◽  
A. V. Patil ◽  
D. D. Mohite
Keyword(s):  
Drug Release ◽  
Oral Drug Delivery ◽  
Drug Carrier ◽  
Amorphous State ◽  
Entrapment Efficiency ◽  
Oral Drug ◽  
Slurry Method ◽  
Span 60

Proniosomes of ritonavir were prepared by slurry method using Span 60, maltodextrin and cholesterol. The ratio of concentration of Span 60 to cholesterol was altered while keeping concentration of drug and maltodextrin constant. Prepared formulations were studied for micromeritic properties, entrapment efficiency, particle size, surface morphology and in vitro drug release. Micromeritic properties of all formulations increased as compared to drug and carrier alone. Entrapment efficiency was observed greater than 90 % and drug release was found to be sustained for upto 12 hours in case of all formulations. Pure drug, carrier and optimized batch F2 was further characterized for SEM, DSC, XRD. Results revealed transformation of crystalline drug to amorphous state. Stability studies performed at refrigeration and room temperature showed that proniosomes were stable at both the temperatures. It is concluded that proniosomes act as efficient and promising carrier system for ritonavir.

Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

2020 ◽  
Vol 12 (2) ◽  
pp. 4474-4491
Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Tem Analysis ◽  
In Vitro Drug Release ◽  
Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

Polymeric Nanoparticles for Brain Drug Delivery - A Review

2020 ◽  
Vol 21 (9) ◽  
pp. 649-660
Author(s):  
Subashini Raman ◽  
Syed Mahmood ◽  
Ayah R. Hilles ◽  
Md Noushad Javed ◽  
Motia Azmana ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Surface Modification ◽  
Polymeric Nanoparticles ◽  
Drug Loading ◽  
Preparation Methods ◽  
Brain Drug Delivery ◽  
Polymeric Nanoparticle ◽  
Relationship Of ◽  
The Relationship ◽  
The Brain

Background: Blood-brain barrier (BBB) plays a most hindering role in drug delivery to the brain. Recent research comes out with the nanoparticles approach, is continuously working towards improving the delivery to the brain. Currently, polymeric nanoparticle is extensively involved in many therapies for spatial and temporal targeted areas delivery. Methods: We did a non-systematic review, and the literature was searched in Google, Science Direct and PubMed. An overview is provided for the formulation of polymeric nanoparticles using different methods, effect of surface modification on the nanoparticle properties with types of polymeric nanoparticles and preparation methods. An account of different nanomedicine employed with therapeutic agent to cross the BBB alone with biodistribution of the drugs. Results: We found that various types of polymeric nanoparticle systems are available and they prosper in delivering the therapeutic amount of the drug to the targeted area. The effect of physicochemical properties on nanoformulation includes change in their size, shape, elasticity, surface charge and hydrophobicity. Surface modification of polymers or nanocarriers is also vital in the formulation of nanoparticles to enhance targeting efficiency to the brain. Conclusion: More standardized methods for the preparation of nanoparticles and to assess the relationship of surface modification on drug delivery. While the preparation and its output like drug loading, particle size, and charge, permeation is always conflicted, so it requires more attention for the acceptance of nanoparticles for brain delivery.

scholarly journals Long-Acting Risperidone Dual Control System: Preparation, Characterization and Evaluation In Vitro and In Vivo

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1210
Author(s):  
Xieguo Yan ◽  
Shiqiang Wang ◽  
Kaoxiang Sun
Keyword(s):  
Drug Loading ◽  
Entrapment Efficiency ◽  
In Vitro Dissolution ◽  
Dissolution Behavior ◽  
In Vivo Evaluation ◽  
Long Term Treatment ◽  
Long Acting

Schizophrenia, a psychiatric disorder, requires long-term treatment; however, large fluctuations in blood drug concentration increase the risk of adverse reactions. We prepared a long-term risperidone (RIS) implantation system that can stabilize RIS release and established in-vitro and in-vivo evaluation systems. Cumulative release, drug loading, and entrapment efficiency were used as evaluation indicators to evaluate the effects of different pore formers, polymer ratios, porogen concentrations, and oil–water ratios on a RIS implant (RIS-IM). We also built a mathematical model to identify the optimized formulation by stepwise regression. We also assessed the crystalline changes, residual solvents, solubility and stability after sterilization, in-vivo polymer degradation, pharmacokinetics, and tissue inflammation in the case of the optimized formulation. The surface of the optimized RIS microspheres was small and hollow with 134.4 ± 3.5 µm particle size, 1.60 SPAN, 46.7% ± 2.3% implant drug loading, and 93.4% entrapment efficiency. The in-vitro dissolution behavior of RIS-IM had zero-order kinetics and stable blood concentration; no lag time was released for over three months. Furthermore, the RIS-IM was not only non-irritating to tissues but also had good biocompatibility and product stability. Long-acting RIS-IMs with microspheres and film coatings can provide a new avenue for treating schizophrenia.

scholarly journals Development of In Situ Self-Assembly Nanoparticles to Encapsulate Lopinavir and Ritonavir for Long-Acting Subcutaneous Injection

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 904
Author(s):  
Irin Tanaudommongkon ◽  
Asama Tanaudommongkon ◽  
Xiaowei Dong
Keyword(s):  
Sustained Release ◽  
Trough Concentration ◽  
Self Assembly ◽  
Subcutaneous Injection ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Long Acting

Most antiretroviral medications for human immunodeficiency virus treatment and prevention require high levels of patient adherence, such that medications need to be administered daily without missing doses. Here, a long-acting subcutaneous injection of lopinavir (LPV) in combination with ritonavir (RTV) using in situ self-assembly nanoparticles (ISNPs) was developed to potentially overcome adherence barriers. The ISNP approach can improve the pharmacokinetic profiles of the drugs. The ISNPs were characterized in terms of particle size, drug entrapment efficiency, drug loading, in vitro release study, and in vivo pharmacokinetic study. LPV/RTV ISNPs were 167.8 nm in size, with a polydispersity index of less than 0.35. The entrapment efficiency was over 98% for both LPV and RTV, with drug loadings of 25% LPV and 6.3% RTV. A slow release rate of LPV was observed at about 20% on day 5, followed by a sustained release beyond 14 days. RTV released faster than LPV in the first 5 days and slower than LPV thereafter. LPV trough concentration remained above 160 ng/mL and RTV trough concentration was above 50 ng/mL after 6 days with one subcutaneous injection. Overall, the ISNP-based LPV/RTV injection showed sustained release profiles in both in vitro and in vivo studies.

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.

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