Surface Modification of Cisplatin-Complexed Gold Nanoparticles and Its Influence on Colloidal Stability, Drug Loading, and Drug Release

The development of various magnetically-responsive nanostructures is of great importance in biomedicine. The controlled assembly of many small superparamagnetic nanocrystals into large multi-core clusters is needed for effective magnetic drug delivery. Here, we present a novel one-pot method for the preparation of multi-core clusters for drug delivery (i.e., magnetic nanocarriers). The method is based on hot homogenization of a hydrophobic phase containing a nonpolar surfactant into an aqueous phase, using ultrasonication. The solvent-free hydrophobic phase that contained tetradecan-1-ol, γ-Fe2O3 nanocrystals, orlistat, and surfactant was dispersed into a warm aqueous surfactant solution, with the formation of small droplets. Then, a pre-cooled aqueous phase was added for rapid cooling and the formation of solid magnetic nanocarriers. Two different nonpolar surfactants, polyethylene glycol dodecyl ether (B4) and our own N1,N1-dimethyl-N2-(tricosan-12-yl)ethane-1,2-diamine (SP11), were investigated for the preparation of MC-B4 and MC-SP11 magnetic nanocarriers, respectively. The nanocarriers formed were of spherical shape, with mean hydrodynamic sizes <160 nm, good colloidal stability, and high drug loading (7.65 wt.%). The MC-B4 nanocarriers showed prolonged drug release, while no drug release was seen for the MC-SP11 nanocarriers over the same time frame. Thus, the selection of a nonpolar surfactant for preparation of magnetic nanocarriers is crucial to enable drug release from nanocarrier.

Download Full-text

5-Fluorouracil-Impregnated PLGA Coated Gold Nanoparticles for Augmented Delivery to Lung Cancer: in vitro Investigations

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520622666211224103110 ◽

2021 ◽

Vol 22 ◽

Author(s):

Rashmi Gupta ◽

Leena Vishwakarma ◽

Sunil Kant Guleri ◽

Gourav Kumar

Keyword(s):

Lung Cancer ◽

Gold Nanoparticles ◽

Drug Release ◽

Release Kinetics ◽

Drug Loading ◽

A549 Cells ◽

Double Emulsion ◽

Zero Order Release ◽

Reduced Toxicity

Background and Objective: The study aimed to investigate the augmented cytotoxic effects of polymer-coated (poly-lactic-co-glycolic acid-PLGA) gold nanoparticles (GNPs) carrying 5-fluorouracil (5-FU) in the management of lung cancer. Materials and Methods: In this study, several formulations were prepared using a double emulsion (water-oil-water) method and evaluated for drug release behavior, compatibility, cell line toxicity (A549), and apoptosis assessment. Results: Characterization results showed spherical polydispersed particles with size 29.11-178.21 nm, polydispersity index (PDI) 0.191-292, and zeta potential (ZP) 11.19-29.21 (-mV), respectively. The optimized polymer-coated 5-FU loaded gold nanoparticles (PFGNPs) illustrated a maximum drug loading (93.09 ± 10.75%) compared to others. The percent cumulative drug release of polymer-coated 5-FU loaded nanoparticles (PFNPs), 5-FU loaded gold nanoparticles (FGNPs), (PFGNPs) and 5-FU solution were 47.87± 1.5, 41.09±1.8, 56.31±1.05, and 98.8±4.2%, respectively, over 10 h. following zero-order release kinetics (except 5-FU solution). From the MTT results, the cytotoxic effect of PFGNPs on the A549 cells was 82.89 % compared to the 5-FU solution (74.91 %). EGFR and KRAS gene expression analysis under the influence of PFNPs, FGNPs, PFGNPs, and 5-FU was studied and observed maximum potency for PFNPs. Conclusion: PLGA coated biogenic gold nanoparticles have a combined effect to achieve high drug loading, sustained delivery, improved efficacy, and enhanced permeation. Conclusively, the approach may be promising to control lung cancer with reduced toxicity and improved efficacy.

Download Full-text

Gold embedded chitosan nanoparticles with cell membrane mimetic polymer coating for pH-sensitive controlled drug release and cellular fluorescence imaging

Journal of Biomaterials Applications ◽

10.1177/0885328220952594 ◽

2020 ◽

pp. 088532822095259

Author(s):

Ke Ma ◽

Yongbin Cheng ◽

Xinran Wei ◽

Daijun Chen ◽

Xiaoli Zhao ◽

...

Keyword(s):

Drug Release ◽

Fluorescence Imaging ◽

Colloidal Stability ◽

Drug Loading ◽

Tumor Therapy ◽

Chitosan Nanoparticles ◽

Fluorescence Emission ◽

Controlled Drug Release ◽

Ph Sensitive ◽

One Pot

In this work, gold embedded chitosan nanoparticles (Au@CS NPs) were fabricated by a one-pot method. The benzaldehyde-terminated poly[(2-methacryloyloxy) ethyl phosphorylcholine] (PMPC) was applied to modification of the gold doped chitosan nanoparticles. The obtained Au@CS-PMPC NPs had the diameter of 135 nm with a narrow distribution. The size of the Au@CS-PMPC NPs, as well as the size of the embedded gold NPs, might be well-controlled by adjusting the feeding ratio between chitosan and HAuCl4. Furthermore, the Au@CS-PMPC NPs showed increased colloidal stability, high drug loading content, pH-responsive drug release, excellent biocompatibility and bright fluorescence emission. The results demonstrated that Au@CS-PMPC NPs showed a great potential for tumor therapy via the combination advantages of pH-sensitive controlled drug release and cellular fluorescence imaging.

Download Full-text

5-Fluorouracil Loaded Biogenic and Albumin Capped Gold Nanoparticles Using Bacterial Enzyme—In Vitro-In Silico Gastroplus® Simulation and Prediction

Processes ◽

10.3390/pr8121579 ◽

2020 ◽

Vol 8 (12) ◽

pp. 1579

Author(s):

Wael A. Mahdi ◽

Afzal Hussain ◽

Mohd. Ramzan

Keyword(s):

Gold Nanoparticles ◽

Drug Release ◽

Zeta Potential ◽

In Silico ◽

Drug Loading ◽

Progressive Increase ◽

Key Factors ◽

Bacterial Enzyme ◽

Mcf 7

The study investigated in situ biosynthesis of albumin capped 5-fluorouracil (5-FU) loaded gold nanoparticles (NPs) using bacterial extract for enhanced efficacy against MCF-7 and in silico prediction using a GastroPlus® software. The optimized formulations were characterized for morphology, size, zeta potential, drug loading (%DL) and entrapment (%EE), compatibility, in vitro drug release, in vitro hemolysis, cellular toxicity and apoptosis studies. The results exhibited highly dispersed albumin capped mono-metallic stable NPs. Spherical size, negative zeta potential and polydispersity index were in range of 38.25–249.62 nm, 18.18–29.87 mV and 0.11–0.283, respectively. F11, F7 and F3 showed a progressive increase in %DL and %EE with increased concentration of the cellular lysate (100% > 50% > 10%). The drug release was relatively extended over 48 h as compared to drug solution (96.64% release within 5 h). The hemolysis result ensured hemocompatibility (<14%) at the explored concentration. The biogenic F11 was more cytotoxic (81.99% inhibition by F11 and 72.04% by pure 5-FU) to the MCF-7 cell lines as compared to others which may be attributed to the preferential accumulation by the tumor cell and capped albumin as the source of energy to the cancer cells. Finally, GastroPlus® predicted the key factors responsible for improved pharmacokinetics parameters and regional absorption from various segments of human intestine. Thus, the approach can be more efficacious and suitable to control breast cancer when administered transdermally or orally.

Download Full-text

Effect of surface modification with various thiol compounds on colloidal stability of gold nanoparticles

Applied Organometallic Chemistry ◽

10.1002/aoc.4079 ◽

2017 ◽

Vol 32 (2) ◽

Cited By ~ 12

Author(s):

Mahsa Mazloomi‐Rezvani ◽

Mehdi Salami‐Kalajahi ◽

Hossein Roghani‐Mamaqani ◽

Amin Pirayesh

Keyword(s):

Gold Nanoparticles ◽

Surface Modification ◽

Colloidal Stability ◽

Thiol Compounds ◽

Effect Of Surface

Download Full-text

Seed-mediated synthesis and PEG coating of gold nanoparticles for controlling morphology and sizes

MRS Advances ◽

10.1557/adv.2020.416 ◽

2020 ◽

Vol 5 (63) ◽

pp. 3353-3360

Author(s):

Susana Helena Arellano Ramírez ◽

Perla García Casillas ◽

Christian Chapa González

Keyword(s):

Gold Nanoparticles ◽

Polyethylene Glycol ◽

Room Temperature ◽

Colloidal Stability ◽

Infrared Spectrometry ◽

Ammonium Bromide ◽

Chloroauric Acid ◽

Vis Spectroscopy ◽

Seed Mediated ◽

Peg Coating

AbstractA significant area of research is biomedical applications of nanoparticles which involves efforts to control the physicochemical properties through simple and scalable processes. Gold nanoparticles have received considerable attention due to their unique properties that they exhibit based on their morphology. Gold nanospheres (AuNSs) and nanorods (AuNRs) were prepared with a seed-mediated method followed of polyethylene glycol (PEG)-coating. The seeds were prepared with 0.1 M cetyltrimethyl-ammonium bromide (CTAB), 0.005 M chloroauric acid (HAuCl4), and 0.01 M sodium borohydride (NaBH4) solution. Gold nanoparticles with spherical morphology was achieved by growth by aggregation at room temperature, while to achieve the rod morphology 0.1 M silver nitrate (AgNO3) and 0.1 M ascorbic acid solution were added. The gold nanoparticles obtained by the seed-mediated synthesis have spherical or rod shapes, depending on the experimental conditions, and a uniform particle size. Surface functionalization was developed using polyethylene glycol. Morphology, and size distribution of AuNPs were evaluated by Field Emission Scanning Electron Microscopy. The average size of AuNSs, and AuNRs was 7.85nm and 7.96 x 31.47nm respectively. Fourier transform infrared spectrometry was performed to corroborate the presence of PEG in the AuNPs surface. Additionally, suspensions of AuNSs and AuNRs were evaluated by UV-Vis spectroscopy. Gold nanoparticles were stored for several days at room temperature and it was observed that the colloidal stability increased once gold nanoparticles were coated with PEG due to the shield formed in the surface of the NPs and the increase in size which were 9.65±1.90 nm of diameter for AuNSs and for AuNRs were 29.03±5.88 and 8.39±1.02 nm for length and transverse axis, respectively.

Download Full-text

Determination of Drug Loading Efficiency and Drug Release of Loperamide from Polymeric Nanocarriers

10.26226/morressier.57d6b2b6d462b8028d88dafe ◽

2016 ◽

Author(s):

Javier Morales

Keyword(s):

Drug Release ◽

Drug Loading ◽

Polymeric Nanocarriers ◽

Loading Efficiency ◽

Drug Loading Efficiency

Download Full-text

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

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2019.12.2.5 ◽

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

Download Full-text

Formulating SLN and NLC as Innovative Drug Delivery Systems for Non-Invasive Routes of Drug Administration

Current Medicinal Chemistry ◽

10.2174/0929867326666190624155938 ◽

2020 ◽

Vol 27 (22) ◽

pp. 3623-3656 ◽

Cited By ~ 1

Author(s):

Bruno Fonseca-Santos ◽

Patrícia Bento Silva ◽

Roberta Balansin Rigon ◽

Mariana Rillo Sato ◽

Marlus Chorilli

Keyword(s):

Drug Delivery ◽

Particle Size ◽

Drug Release ◽

Drug Loading ◽

Average Particle Size ◽

Delivery Systems ◽

Average Particle ◽

Minor Importance ◽

Routes Of Administration ◽

Non Invasive

Colloidal carriers diverge depending on their composition, ability to incorporate drugs and applicability, but the common feature is the small average particle size. Among the carriers with the potential nanostructured drug delivery application there are SLN and NLC. These nanostructured systems consist of complex lipids and highly purified mixtures of glycerides having varying particle size. Also, these systems have shown physical stability, protection capacity of unstable drugs, release control ability, excellent tolerability, possibility of vectorization, and no reported production problems related to large-scale. Several production procedures can be applied to achieve high association efficiency between the bioactive and the carrier, depending on the physicochemical properties of both, as well as on the production procedure applied. The whole set of unique advantages such as enhanced drug loading capacity, prevention of drug expulsion, leads to more flexibility for modulation of drug release and makes Lipid-based nanocarriers (LNCs) versatile delivery system for various routes of administration. The route of administration has a significant impact on the therapeutic outcome of a drug. Thus, the non-invasive routes, which were of minor importance as parts of drug delivery in the past, have assumed added importance drugs, proteins, peptides and biopharmaceuticals drug delivery and these include nasal, buccal, vaginal and transdermal routes. The objective of this paper is to present the state of the art concerning the application of the lipid nanocarriers designated for non-invasive routes of administration. In this manner, this review presents an innovative technological platform to develop nanostructured delivery systems with great versatility of application in non-invasive routes of administration and targeting drug release.

Download Full-text

Mesoporous Silica Molecular Sieve based Nanocarriers: Transpiring Drug Dissolution Research

Current Pharmaceutical Design ◽

10.2174/1381612822666161026162005 ◽

2017 ◽

Vol 23 (3) ◽

pp. 467-480 ◽

Cited By ~ 8

Author(s):

Satyanarayan Pattnaik ◽

Kamla Pathak

Keyword(s):

Drug Release ◽

Mesoporous Silica ◽

Molecular Sieves ◽

Release Kinetics ◽

Drug Loading ◽

Scale Up ◽

Water Soluble ◽

Drug Dissolution ◽

Water Soluble Drugs ◽

Loading Methods

Background: Improvement of oral bioavailability through enhancement of dissolution for poorly soluble drugs has been a very promising approach. Recently, mesoporous silica based molecular sieves have demonstrated excellent properties to enhance the dissolution velocity of poorly water-soluble drugs. Description: Current research in this area is focused on investigating the factors influencing the drug release from these carriers, the kinetics of drug release and manufacturing approaches to scale-up production for commercial manufacture. Conclusion: This comprehensive review provides an overview of different methods adopted for synthesis of mesoporous materials, influence of processing factors on properties of these materials and drug loading methods. The drug release kinetics from mesoporous silica systems, the manufacturability and stability of these formulations are reviewed. Finally, the safety and biocompatibility issues related to these silica based materials are discussed.

Download Full-text