Nanocrystals- A substantial platform for drug delivery applications.

2021 ◽  
Vol 12 ◽  
Author(s):  
Akanksha Patel ◽  
Abhay Dharamsi

Abstract: Poor solubility of a drug is one of the major concerns in drug delivery. Many strategies have been employed for solving this problem, but there are still some deficiencies with current strategies, such as low drug loading, high toxicity, poor stability, potential drug loss during storage and complex manufacturing method. By formulating nanocrystals, problems associated with the delivery of drugs with low water or lipid solubility can be addressed. Unlike polymeric nanoparticles and lipidic nanoparticles, they are not a reservoir or matrix system. Nanocrystals are colloidal suspensions of nanosized particles stabilized by polymeric or electrostatic stabilization. They can be prepared by Top-down or Bottom-up approaches. Some of the methods for the preparation of nanocrystals are nanoprecipitation, media milling, high-pressure homogenization, emulsions and microemulsions as templates, supercritical fluid technology and co-grinding. They can be used for oral, intravenous, ocular, inhalation, intramuscular drug delivery and drug targeting.

2020 ◽  
Vol 21 (9) ◽  
pp. 649-660
Author(s):  
Subashini Raman ◽  
Syed Mahmood ◽  
Ayah R. Hilles ◽  
Md Noushad Javed ◽  
Motia Azmana ◽  
...  

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.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 912
Author(s):  
Guzmán Carissimi ◽  
Mercedes G. Montalbán ◽  
Gloria Víllora ◽  
Andreas Barth

Nanotechnology has enabled the development of novel therapeutic strategies such as targeted nanodrug delivery systems, control and stimulus-responsive release mechanisms, and the production of theranostic agents. As a prerequisite for the use of nanoparticles as drug delivery systems, the amount of loaded drug must be precisely quantified, a task for which two approaches are currently used. However, both approaches suffer from the inefficiencies of drug extraction and of the solid-liquid separation process, as well as from dilution errors. This work describes a new, reliable, and simple method for direct drug quantification in polymeric nanoparticles using attenuated total reflection Fourier transform infrared spectroscopy, which can be adapted for a wide variety of drug delivery systems. Silk fibroin nanoparticles and naringenin were used as model polymeric nanoparticle carrier and drug, respectively. The specificity, linearity, detection limit, precision, and accuracy of the spectroscopic approach were determined in order to validate the method. A good linear relation was observed within 0.00 to 7.89% of naringenin relative mass with an R2 of 0.973. The accuracy was determined by the spike and recovery method. The results showed an average 104% recovery. The limit of detection and limit of quantification of the drug loading content were determined to be 0.3 and 1.0%, respectively. The method’s robustness is demonstrated by the notable similarities between the calibrations carried out using two different equipment setups at two different institutions.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 827 ◽  
Author(s):  
Victor Lotocki ◽  
Ashok Kakkar

Delivering active pharmaceutical agents to disease sites using soft polymeric nanoparticles continues to be a topical area of research. It is becoming increasingly evident that the composition of amphiphilic macromolecules plays a significant role in developing efficient nanoformulations. Branched architectures with asymmetric polymeric arms emanating from a central core junction have provided a pivotal venue to tailor their key parameters. The build-up of miktoarm stars offers vast polymer arm tunability, aiding in the development of macromolecules with adjustable properties, and allows facile inclusion of endogenous stimulus-responsive entities. Miktoarm star-based micelles have been demonstrated to exhibit denser coronae, very low critical micelle concentrations, high drug loading contents, and sustained drug release profiles. With significant advances in chemical methodologies, synthetic articulation of miktoarm polymer architecture, and determination of their structure-property relationships, are now becoming streamlined. This is helping advance their implementation into formulating efficient therapeutic interventions. This review brings into focus the important discoveries in the syntheses of miktoarm stars of varied compositions, their aqueous self-assembly, and contributions their formulations are making in advancing the field of drug delivery.


2021 ◽  
Vol 27 ◽  
Author(s):  
Mayank Handa ◽  
Ajit Singh ◽  
S.J.S. Flora ◽  
Rahul Shukla

Background: Recent past decades have reported emerging of polymeric nanoparticles as a promising technique for controlled and targeted drug delivery. As nanocarriers, they have high drug loading and delivery to the specific site or targeted cells with an advantage of no drug leakage within en route and unloading of a drug in a sustained fashion at the site. These stimuli-responsive systems are functionalized in dendrimers, metallic nanoparticles, polymeric nanoparticles, liposomal nanoparticles, quantum dots. Purpose of Review: The authors reviewed the potential of smart stimuli-responsive carriers for therapeutic application and their behavior in external or internal stimuli like pH, temperature, redox, light, and magnet. These stimuli-responsive drug delivery systems behave differently in In vitro and In vivo drug release patterns. Stimuli-responsive nanosystems include both hydrophilic and hydrophobic systems. This review highlights the recent development of the physical properties and their application in specific drug delivery. Conclusion: The stimuli (smart, intelligent, programmed) drug delivery systems provide site-specific drug delivery with potential therapy for cancer, neurodegenerative, lifestyle disorders. As development and innovation, the stimuli-responsive based nanocarriers are moving at a fast pace and huge demand for biocompatible and biodegradable responsive polymers for effective and safe delivery.


2015 ◽  
Vol 2015 ◽  
pp. 1-12 ◽  
Author(s):  
Abdalrahim F. A. Aisha ◽  
Amin Malik Shah Abdulmajid ◽  
Zhari Ismail ◽  
Salman A. Alrokayan ◽  
Khalid M. Abu-Salah

Xanthones are a group of oxygenated heterocyclic compounds with anticancer properties, but poor aqueous solubility and low oral bioavailability hinder their therapeutic application. This study sought to prepare a xanthones extract (81%  α-mangostin and 16%  γ-mangostin) in polymeric nanoparticles and to investigate its intracellular delivery and cytotoxicity toward colon cancer cells. The nanoparticles were prepared in Eudragit RL100 and Eudragit RS100 by the nanoprecipitation method at drug loading and entrapment efficiency of 20% and >95%, respectively. Freeze-drying of bulk nanoparticle solutions, using glucose or sucrose as cryoprotectants, allowed the collection of nanoparticles at >95% yield. Solubility of the xanthones extract was improved from 0.1 µg/mL to 1250 µg/mL. Transmission electron microscopy (TEM) and dynamic light scattering (DLS) of the freeze-dried final formulation showed the presence of cationic round nanoparticles, with particle size in the range of 32–130 nm. Scanning electron microscopy (SEM) showed the presence of nanospheres, and Fourier transform infrared (FTIR) spectroscopy indicated intermolecular interaction of xanthones with Eudragit polymers. Cellular uptake of nanoparticles was mediated via endocytosis and indicated intracellular delivery of xanthones associated with potent cytotoxicity (median inhibitory concentration26.3±0.22 µg/mL). Presented results suggest that cationic nanoparticles of xanthones may provide a novel oral drug delivery system for chemoprevention or treatment of intestinal and colon tumors.


Author(s):  
Guzmán Carissimi ◽  
Mercedes G. Montalbán ◽  
Gloria Víllora ◽  
Andreas Barth

Nanotechnology has enabled the development of novel therapeutic strategies such as targeted nanodrug delivery systems, control and stimulus-responsive release mechanisms, and the production of theranostic agents. As a prerequisite for the use of nanoparticles as drug delivery systems, the amount of loaded drug must be precisely quantified, a task for which two approaches are currently used. However, both approaches suffer from the inefficiencies of drug extraction and of the solid-liquid separation process, as well as from dilution errors. This work describes a new, reliable, and simple method for direct drug quantification in polymeric nanoparticles using attenuated total reflection Fourier transform infrared spectroscopy, which can be adapted for a wide variety of drug delivery systems. Silk fibroin nanoparticles and naringenin were used as model polymeric nanoparticle carrier and drug, respectively. The specificity, linearity, detection limit, precision and accuracy of the spectroscopic approach were determined in order to validate the method. A good linear relation was observed within 0.00 to 7.89 % of naringenin relative mass with an R2 of 0.973. The accuracy was determined by the spike and recovery method. Results showed an average 104% recovery. The limit of detection and limit of quantification of the drug loading content were determined to be 0.3 and 1.0 %, respectively. The method's robustness is demonstrated by the notable similarities between the calibrations carried out in two different equipment and institutions.


2020 ◽  
Vol 17 ◽  
Author(s):  
Ozge Esim ◽  
Canan Hascicek

: Currently, despite many active compounds have been introduced to the treatment, cancer remains one of the most vital causes of mortality and reduced quality of life. Conventional cancer treatments may have undesirable consequences due to the continuously differentiating, dynamic and heterogeneous nature of cancer. Recent advances in the field of cancer treatment have promoted the development of several novel nanoformulations. Among them, the lipid coated nanosized drug delivery systems have gained an increasing attention by the researchers in this field owing to the attractive properties such as high stability and biocompatibility, prolonged circulation time, high drug loading capacity and superior in vivo efficacy. They possess the advantages of both the liposomes and polymeric nanoparticles which makes them a chosen one in the field of drug delivery and targeting. Core-shell type lipid-coated nanoparticle systems, which provide the most prominent advantages of both liposomes such as biocompatibility and polymeric/inorganic nanoparticles such as mechanic properties, offer a new approach to cancer treatment. This review discusses design and production procedures used to prepare lipid-coated nanoparticle drug delivery systems, their advantages and multifunctional role in cancer therapy and diagnosis, as well as the applications they have been used in.


2020 ◽  
Vol 08 ◽  
Author(s):  
Sweet Naskar ◽  
Sanjoy Kumar Das ◽  
Suraj Sharma ◽  
Ketousetuo Kuotsu

: Poly (lactic-co-glycolic acid) (PLGA) is one of the versatile synthetic polymer comprehensively used in the pharmaceutical sectorbecause of its biocompatibility and biodegradability.These benefits lead to its application in the area of nanoparticles (NPs) for the drug delivery over the thirty years. This article offers to climb a general study of the different poly (lactic-co-glycolic acid) nanoparticles (PNPs) preparation methods such as emulsification-solvent evaporation, coacervation, emulsification solvent diffusion, dialysis, emulsification reverse salting out, spray drying nanoprecipitation, and supercritical fluid technology, from the methodological point of view.The physicochemical behavior of PNPs including morphology, drug loading, particle size and its distribution, surface charge, drug release, stability as well as cytotoxicity study and cellular uptake are briefly discussed. This survey additionally coordinates to bring a layout of the significant uses of PNPs in different drug delivery system over the three decades. At last, surface modifications of PNPs and PLGA nanocomplexes (NCs) are additionally examined.


RSC Advances ◽  
2021 ◽  
Vol 11 (31) ◽  
pp. 18809-18817
Author(s):  
Ali Bina ◽  
Heidar Raissi ◽  
Hassan Hashemzadeh ◽  
Farzaneh Farzad

Polymeric nanoparticles have emerged as efficient carriers for anticancer drug delivery because they can improve the solubility of hydrophobic drugs and also can increase the bio-distribution of drugs throughout the bloodstream.


2021 ◽  
pp. 11-14
Author(s):  
Pallav Kaushik Deshpande ◽  
Ragini Gothalwal

Most of the active phytoconstituents under development are poorly water soluble or have poor bioavailability . Nanotechnology is an approach to overcome the challenges of conventional drug delivery systems and limitations of phytochemicals. Solid Lipid nanoparticles show interesting features concerning therapeutic purposes. The main advantage is that they are prepared with physiologically well-tolerated lipids.Solid Lipid Nanoparticles (SLNs) as novel lipid based nanocarriers with size range between 10 to 1000nm. SLNs were introduced to overcome problems of polymeric nanoparticles.In present research formulation and evaluation of nanoparticles with ethanolic extract of two plants Celastrus paniculatus and Bacopa monnieri along with Donepezil as a standard drug was undertaken here for the production methods for preparation of SLNs, and pharmaceutical approach of SLNs in drug delivery . The focus of nanoparticle design over the years has evolved toward more complex nanoscopic core–shell architecture using a single delivery system to combine multiple functionalities within nanoparticles which combine the mechanical advantages of biodegradable polymeric nanoparticles and biomimetic advantages of liposomes, have emerged as a robust and promising delivery platform. Solid liquid nanoparticles having plant extracts were successfully formulated and characterized for their stability.A biodegradable polymeric core is surrounded by a shell composed of layer(s) of phospholipids. This architecture can provide advantages such as controllable particle size, surface functionality, high drug loading, entrapment of multiple therapeutic agents, drug release profile,and good serum stability of phytochemicals


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