scholarly journals Recent developments in nano micelles as drug delivery system

2020 ◽  
Vol 11 (1) ◽  
pp. 176-184
Author(s):  
Pooja Mallya ◽  
Gowda D V ◽  
Mahendran B ◽  
Bhavya M V ◽  
Vikas Jain
Keyword(s):  
Drug Delivery ◽  
Colloidal Particles ◽  
Polymeric Micelles ◽  
Aggregation Number ◽  
Drug Loading ◽  
Polymer Concentration ◽  
Therapeutic Interventions ◽  
Solution Viscosity ◽  
Hydrophobic Core ◽  
Amphiphilic Copolymers

Targeting of the drug directly to the cells, tissues, or organs with no impact on healthy cells is a challenge. In the current era, it's been made possible by therapeutic interventions. The novel drug delivery systems such as nano particulates, liposomes, aquasomes, phytosomes, dendrimers, nano sponges, nano micelles are developed. Nano micelles are developed for efficient targeting and are currently in trend as therapeutic carriers of water-insoluble drugs. Micelles are self-assembling Nano-sized colloidal particles with a hydrophobic core and hydrophilic shell. Among the micelle-forming compounds, amphiphilic copolymers, i.e., polymers consisting of hydrophobic block and hydrophilic block, are gaining increasing attention. Polymeric micelles possess high stability both in vitro and in vivo with good biocompatibility. Nano micelles are used widely because of the smaller size range of 10 to 100nm, with greater drug loading capacity. Advantages over other dosage forms include solubilization of poorly soluble drugs, sustained release, protection of drugs from degradation and metabolism. The property discussed includes CMC, size, and aggregation number, and stability. CMC is the minimum polymer concentration required for micelle formation. Aggregation number (Nₐ) is the number of polymeric chains required to form micelles, and it ranges between tens to hundreds. Thermodynamic stability is based on size, the optical clarity of solution, viscosity, and surface tension. Kinetic stability accounts for micellar integrity. This review will discuss some recent trends in using micelles as pharmaceutical carriers such as to deliver drugs in conditions such as TB, cancer, ocular complications, etc.

Macromolecular engineering and stimulus response in the design of advanced drug delivery systems

MRS Bulletin ◽  
2010 ◽  
Vol 35 (9) ◽  
pp. 665-672 ◽  
Author(s):  
Christine Jérôme
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Colloidal Particles ◽  
Polymeric Micelles ◽  
Complex Structure ◽  
Delivery Systems ◽  
Target Cells ◽  
Amphiphilic Copolymers ◽  
Stimuli Responsive ◽  
Research Activity

Extensive research activity is currently devoted to controlled drug delivery systems, mainly as nano-sized particles. Although biocompatible and (bio)degradable polymers play a key role in this field, their shaping into colloidal particles (e.g., polymeric micelles and nanoparticles) usually requires the proper design of amphiphilic copolymers as effective stabilizers. Strategies for synthesizing these copolymers that preserve the intrinsic properties of the constitutive polymers are discussed in this article. Synthesis of amphiphilic copolymers with a more complex structure and endowed with functionality is also considered, with the purpose of enhancing the performance of the nanocarriers. The focus is increasingly on nanocarriers of the third generation, which resist coalescence and elimination by the immune system, and which are readily incorporated into chosen target cells. The more recent quest is for smart nanocarriers that exhibit the additional capacity of being stimuli-responsive.

scholarly journals Liposomal drug delivery system as an effective treatment approach for lung cancer

2020 ◽  
Vol 10 (3-s) ◽  
pp. 367-370
Author(s):  
Kinjal Patel ◽  
Devanshi Patel
Keyword(s):  
Lung Cancer ◽  
Drug Delivery ◽  
Drug Loading ◽  
Chemotherapeutic Agents ◽  
The Body ◽  
Therapeutic Interventions ◽  
Target Delivery ◽  
Liposomal Drug ◽  
Cancer Management ◽  
Important Field

Worldwide, cancer is one of the leading causes of mortality and cancer rates are set to increase at alarming rate globally. There are various types of cancer in which the leading type is the lung cancer.   In recent years lipid-based carriers, such as liposomes, have successfully encapsulated chemotherapeutic agents ameliorating some toxicity issues, while enhancing the overall therapeutic activity in cancer patients. In addition to this, nanomaterials can help to improved half-life in the body, morphology, for increased drug loading and many other ways. The survey discussed in this review will lead the anticancer therapy and cancer management which will provide the platform to the next generation.  Therefore, this critical review includes the therapeutic interventions, liposomes target delivery, active and passive drug loading. Finally, we attempt to summarize the current challenges in nanotherapeutics and provide an outlook on the future of this important field. Keywords: Drug Delivery, Liposomes target Delivery, Nanostructures, Drug loading

Skeletal-Targeted, Osteolytic-Responsive Drug Delivery System Improves Anti-Tumor Efficacy in Multiple Myeloma.

Blood ◽  
2012 ◽  
Vol 120 (21) ◽  
pp. 3155-3155
Author(s):  
Xuli Wang ◽  
Ye Yang ◽  
Scott Miller ◽  
Fenghuang Zhan
Keyword(s):  
Drug Delivery ◽  
Multiple Myeloma ◽  
Polymeric Micelles ◽  
Conflicts Of Interest ◽  
Drug Loading ◽  
Bone Matrix ◽  
Cathepsin K ◽  
Laser Scanning Microscopy ◽  
Confocal Laser ◽  
Tumor Inhibition

Abstract Abstract 3155 Background: Multiple myeloma (MM) cells often directly or indirectly induce the formation of osteoclasts, which enhance bone resorption by increasing secretion of a key protease (cathepsin K) to degrade bone matrix, leading to osteolytic lesions and serious skeletal complications. Hence, bone-targeted, osteolytic-responsive therapeutic modalities are greatly needed to improve clinical outcomes for MM. Methods and Results: A tri-block copolymer of peptide, poly(ethylene glycol) and poly(trimethylene carbonate) (Pep-b-PEG-b-PTMC) has been synthesized as a nanocarrier to improve treatment for MM. The functional peptide with the sequence of CKGHPGGPQAsp8 was designed to possess a bone tropism octapeptide (Asp8), a cathepsin K (CTSK)-cleavable substrate (HPGGPQ), multiple cationic residues and a terminal cysteine for site-specific conjugation. Maleimide-terminated diblock copolymer of PEG-b-PTMC was readily functionalized with the peptide to obtain Pep-b-PEG-b-PTMC that can spontaneously form micelles with the size of 75 nm in diameter. Sixty-six % of polymeric micelles were able to bind to hydroxyl apatite, showing high bone binding capability. The nanoparticles exhibited a negative-to-positive charge conversional profile upon exposure to cathepsin K, an overexpressed enzyme in osteolytic microenvironments. By using doxorubicin as a model drug, Pep-b-PEG-b-PTM showed 7.5 ± 0.5 % and 22.7 ± 1.5% for drug loading content and drug loading efficiency, respectively. More importantly, a unique characteristic of on-demand charge-conversional behaviour in a cathepsin K-rich condition led to enhanced cellular uptake of the nanotherapeutics, as demonstrated by confocal laser scanning microscopy. Enhanced tumor inhibition was observed in 5TGM1 MM cells when nanoparticles were pre-treated with 150 nM cathepsin K, demonstrating enzyme-triggered improved therapy. Efficacy of free DOX or DOX-loaded NPs in 5TGM1 mice bearing myeloma was further preliminarily tested. 5TGM1 mice bearing myeloma were established through injection of 5TGM1 cells (1 × 106 cells in 100 μL PBS) via tail vein, and tumor was allowed to grow for a week before initiating treatment study. Mice (n=3) were injected twice weekly with different therapeutic formulations at equivalent DOX dose (0.75 mg/Kg) or PBS. Tumor burden in the mice was monitored by ELISA measurements of serum IgG2b. Drug-loaded nanoparticles from Pep-b-PEG-b-PTMC were more efficacious in terms of mice survival rate and tumor inhibition when compared to the groups with non-targeted nanoparticles from mPEG-PTMC, free DOX or PBS controls. This improved drug efficacy may be attributed to more selective delivery of DOX to bone metastatic tissues and/or responsiveness of the nanoparticles to cathepsin K, thus improving tumor uptake of DOX, enhancing therapeutic efficacy in terms of tumor reduction as well as MM mouse survival. Conclusions: The promising results from this study may prompt the development of bone-targeted, enzyme-triggered drug delivery systems to improve their affinity to skeletal tissues, enhance selectivity for osteolytic regions and improve efficacy of anti-cancer agents, thus facilitating the development of effective nanotherapeutic modalities for multiple myeloma. Disclosures: No relevant conflicts of interest to declare.

scholarly journals Preparation and characterization of N-benzyl-N,O-succinyl chitosan polymeric micelles for solubilization of poorly soluble non-steroidal anti-inflammatory drugs

2017 ◽  
Vol 16 (10) ◽  
pp. 2349-2357
Author(s):  
Thisirak Woraphatphadung ◽  
Warayuth Sajomsang ◽  
Theerasak Rojanarata ◽  
Prasert Akkaramongkolporn ◽  
Tanasait Ngawhirunpat ◽  
...  
Keyword(s):  
Particle Size ◽  
Surface Charge ◽  
Polymeric Micelles ◽  
Rank Order ◽  
Drug Loading ◽  
Polymer Concentration ◽  
Water Soluble ◽  
Loading Efficiency ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Purpose: To investigate the solubilization of poorly water-soluble non-steroidal  anti-inflammatory drugs (NSAIDs) in N-benzyl-N,O-succinyl chitosan (BSCS)  polymeric micellesMethods: BSCS was synthesized by reductive amination and succinylation,  respectively. NSAIDs; meloxicam (MX), piroxicam (PRX), ketoprofen (KP) and indomethacin (IND) were entrapped in the hydrophobic inner cores by evaporation method. The effects of drug structure on loading efficiency, particle size and surface charge of micelles were investigated.Results: The critical micelle concentration of BSCS micelles was 0.0385 mg/mL and cytotoxicity on Caco-2 cells depends on the polymer concentration (IC50 = 3.23 ± 0.08 mg/mL). BSCS micelles were able to entrap MX, PRX, KP and IND and also improve the solubility of drugs. Drug loading efficiency was highly dependent on the drug molecules. The drug loading capacity of these BSCS micelles was in the following rank order: KP (282.9 μg/mg) > PRX (200.8 μg/mg) > MX (73.7 μg/mg) > IND (41.2 μg/mg). The highest loading efficiency was observed in KP-loaded BSCS micelles due to the attractive force between phenyl groups of KP and benzyl groups of the polymer. Particle size and surface charge were in the range of 312 - 433 nm and -38 to -41 mV, respectively.Conclusion: BSCS copolymer presents desirable attributes for enhancing the  solubility of hydrophobic drugs. Moreover, BSCS polymeric micelles might be beneficial carrier in a drug delivery system.Keywords: BSCS, polymeric micelles, solubilization, non-steroidal anti-inflammatory drugs

scholarly journals Miktoarm Star Polymers: Branched Architectures in Drug Delivery

Pharmaceutics ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 827 ◽  
Author(s):  
Victor Lotocki ◽  
Ashok Kakkar
Keyword(s):  
Drug Delivery ◽  
Self Assembly ◽  
Polymeric Nanoparticles ◽  
Drug Loading ◽  
Therapeutic Interventions ◽  
Structure Property ◽  
Sustained Drug Release ◽  
Amphiphilic Macromolecules ◽  
Miktoarm Star ◽  
Core Junction

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.

scholarly journals Acid-Responsive Adamantane-Cored Amphiphilic Block Polymers as Platforms for Drug Delivery

Nanomaterials ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 188
Author(s):  
Weiqiu Wen ◽  
Chong Guo ◽  
Jianwei Guo
Keyword(s):  
Drug Delivery ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Controlled Drug Release ◽  
Polymeric Micelle ◽  
Monomethyl Ether ◽  
Particle Sizes ◽  
Anticancer Efficacy ◽  
Decrease Rate ◽  
Anticancer Drug Delivery

Four-arm star-shaped (denoted as ‘S’) polymer adamantane-[poly(lactic-co-glycolic acid)-b-poly(N,N’-diethylaminoethyl methacrylate) poly(ethylene glycol) monomethyl ether]4 (S-PLGA-D-P) and its linear (denoted as ‘L’) counterpart (L-PLGA-D-P) were synthesized, then their self-assembled micelles were further developed to be platforms for anticancer drug delivery. Two types of polymeric micelles exhibited strong pH-responsiveness and good drug loading capacity (21.6% for S-PLGA-D-P and 22.9% for L-PLGA-D-P). Using doxorubicin (DOX) as the model drug, their DOX-loaded micelles displayed well controlled drug release behavior (18.5–19.0% of DOX release at pH 7.4 and 77.6–78.8% of DOX release at pH 5.0 within 80 h), good cytocompatibility against NIH-3T3 cells and effective anticancer efficacy against MCF-7 cells. However, the star-shaped polymeric micelles exhibited preferable stability, which was confirmed by the lower critical micelle concentration (CMC 0.0034 mg/mL) and decrease rate of particle sizes after 7 days incubation (3.5%), compared with the linear polymeric micelle L-PLGA-D-P (CMC 0.0070 mg/mL, decrease rate of particle sizes was 9.6%). Overall, these developed polymeric micelles have promising application as drug delivery system in cancer therapy.

scholarly journals Design of Gelatin-Capped Plasmonic-Diatomite Nanoparticles with Enhanced Galunisertib Loading Capacity for Drug Delivery Applications

2021 ◽  
Vol 22 (19) ◽  
pp. 10755
Author(s):  
Chiara Tramontano ◽  
Bruno Miranda ◽  
Giovanna Chianese ◽  
Luca De Stefano ◽  
Carlo Forestiere ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Loading ◽  
Polymer Concentration ◽  
Localized Surface Plasmon ◽  
Loading Capacity ◽  
Predictive Tool ◽  
Optical Modeling ◽  
Hybrid Platform ◽  
Drug Delivery Applications ◽  
First Time

Inorganic diatomite nanoparticles (DNPs) have gained increasing interest as drug delivery systems due to their porous structure, long half-life, thermal and chemical stability. Gold nanoparticles (AuNPs) provide DNPs with intriguing optical features that can be engineered and optimized for sensing and drug delivery applications. In this work, we combine DNPs with gelatin stabilized AuNPs for the development of an optical platform for Galunisertib delivery. To improve the DNP loading capacity, the hybrid platform is capped with gelatin shells of increasing thicknesses. Here, for the first time, full optical modeling of the hybrid system is proposed to monitor both the gelatin generation, degradation, and consequent Galunisertib release by simple spectroscopic measurements. Indeed, the shell thickness is optically estimated as a function of the polymer concentration by exploiting the localized surface plasmon resonance shifts of AuNPs. We simultaneously prove the enhancement of the drug loading capacity of DNPs and that the theoretical modeling represents an efficient predictive tool to design polymer-coated nanocarriers.

scholarly journals Preparation and Evaluation of Eudragit® L100 Nanoparticles LoadedImpregnated with KT Tromethamine Loaded PVA -HEC Insertions forOphthalmic Drug Delivery

2019 ◽  
Vol 9 (4) ◽  
pp. 593-600
Author(s):  
Ghobad Mohammadi ◽  
Shahla Mirzaeei ◽  
Shiva Taghe ◽  
Pardis Mohammadi
Keyword(s):  
Drug Delivery ◽  
Moisture Absorption ◽  
Drug Loading ◽  
Polymer Concentration ◽  
Hydroxyethyl Cellulose ◽  
Moisture Loss ◽  
Physiochemical Parameters ◽  
Ft Ir ◽  
First Time ◽  
Preparation And Evaluation

Purpose: The purpose of the present study was to improve the ocular delivery for ketorolactromethamine (KT) used to treat inflammation of the eye.Methods: Eudragit nanoparticles loaded with KT were prepared and incorporated in polyvinylalcohol (PVA) and hydroxyethyl cellulose (HEC) films. Nanoparticles were characterized byFourier transform-infrared (FT-IR), scanning electron microscopy (SEM). Physicochemicalproperties and encapsulation effciency were investigated for nanoparticles. Also, the insertswere evaluated for their physiochemical parameters like percentage moisture absorption,percentage moisture loss, thickness and folding endurance.Results: Mean particle size and zeta potential were in range of 153.8-217 nm and (-10.8) -(-40.7) mV, respectively. The results show that the use of a surfactant has not led to any majorchange on drug loading. The loading increases with the amount of polymer. The insert had athickness varying from 0.072 ± 0.0098 to 0.0865 ± 0.0035 mm. The thicknesses of the insertsand the folding endurance increased with the total polymer concentration. The physicochemicalproperties showed that the Eudragit® L-100 nanoparticles loaded PVA-HEC films could be aneffective carrier for KT.Conclusion: For the first time, inserts of Eudragit nanoparticles were successfully prepared forophthalmic drug delivery system to prevent frequent drug administration and enhance patientcompliance.<br />

scholarly journals Encapsulation for Cancer Therapy

Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1605 ◽  
Author(s):  
Xavier Montané ◽  
Anna Bajek ◽  
Krzysztof Roszkowski ◽  
Josep M. Montornés ◽  
Marta Giamberini ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Cancer Detection ◽  
Targeted Delivery ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Inorganic Nanoparticles ◽  
Cancer Drug ◽  
Release Mechanism ◽  
Promising Alternative ◽  
Drug Release Mechanism

The current rapid advancement of numerous nanotechnology tools is being employed in treatment of many terminal diseases such as cancer. Nanocapsules (NCs) containing an anti-cancer drug offer a very promising alternative to conventional treatments, mostly due to their targeted delivery and precise action, and thereby they can be used in distinct applications: as biosensors or in medical imaging, allowing for cancer detection as well as agents/carriers in targeted drug delivery. The possibility of using different systems—inorganic nanoparticles, dendrimers, proteins, polymeric micelles, liposomes, carbon nanotubes (CNTs), quantum dots (QDs), biopolymeric nanoparticles and their combinations—offers multiple benefits to early cancer detection as well as controlled drug delivery to specific locations. This review focused on the key and recent progress in the encapsulation of anticancer drugs that include methods of preparation, drug loading and drug release mechanism on the presented nanosystems. Furthermore, the future directions in applications of various nanoparticles are highlighted.

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