Tailoring Nano-copolymer/CNTs Composite and Its Application in Drug Delivery

Author(s):  
M. K. Darwish ◽  
M. S. Said ◽  
A. A. El-Sayed ◽  
R. A. Sobh ◽  
A. A. Abdel Khalek

Abstract This work aimed to overcome the main drawbacks of some essential anticancer drugs as 5-Fluorouracil (5-FU) by controlled loading with novel drug carriers. By a differential microemulsion technique, nanosized particles derived from a copolymer of poly(methyl methacrylate (MMA) and 2-hydroxyethyl methacrylate (HEMA)) with different monomer ratios have been synthesized and used as a drug carrier. Poly(MMA-co-HEMA)/MWCNT nanocomposite was also synthesized using an in-situ microemulsion polymerization technique and used as a 5-FU carrier. Different techniques have characterized these ground-breaking drug delivery systems such as FT-IR, XRD, TEM, TGA, zeta potential, and a particle size analyzer. The effects of monomer feed composition, 5-FU content, and MWCNTs content on morphological and structural properties, in-vitro 5-FU release, and entrapment efficiency (EE%) have been studied. It was noted that the inclusion of MWCNTs in the 5-FU-loaded polymer increases the thermal stability and raises the entrapment efficiency (EE%) to hit 99% at CNTs:5-FU ratio of 2:1. The anticancer drug release from the co-polymeric nanospheres depends on the HEMA ratio, 5-FU/copolymer ratio, CNT/5-FU ratio, and the pH of the medium. The optimized nanocomposite demonstrated higher anti-tumor activity against the cell lines CaCo-2, MCF-7, and HepG-2 and higher cytotoxicity against HepG-2 relative to CaCo-2 and MCF-7.

Author(s):  
Shubham Shitole

Abstract: For the past few years, there has been a considerable research on the basis of Novel drug delivery system, using particulate vesicle systems as such drug carriers for small and large molecules. Nanoparticles, Liposomes, Microspheres, Niosomes, Pronisomes, Ethosomes, Proliposomes have been used as drug carrier in vesicle drug delivery system. Nanotechnology refers to the creation and utilization of materials whose constituents exist at the nanoscale; and, by convention, be up to 100 nm in size.. Nanoparticles are being used for diverse purposes, from medical treatments, using in various branches of industry production such as solar and oxide fuel batteries for energy storage, to wide incorporation into diverse materials of everyday use such as cosmetics or clothes, optical devices, catalytic, bactericidal, electronic, sensor technology, biological labelling and treatment of some cancers. Various polymers have been used in the formation of Nanoparticles. Nanoparticles have been improving the therapeutic effect of drugs and minimize the side effects. Basically, Nanoparticles have been prepared by using various techniques as such dispersion of preformed polymers, polymerization of monomers and ionic gelation or coacervation of hydrophilic polymer. Nanoparticles have been evaluated by using parameters of drug entrapment efficiency, particle shape, drug release study. Keywords: Nanoparticles, Drug, novel, delivery


2019 ◽  
Vol 9 (2) ◽  
pp. 116-133 ◽  
Author(s):  
Anjana Rani ◽  
Sunil Kumar ◽  
Roop K. Khar

Background:Herbal extracts have brilliant in-vitro activity but less in-vivo action in light of their macromolecular size and poor lipid solubility bringing about poor absorption and low bioavailability. These issues can be corrected by designing novel drug delivery systems. Phytosomes provide better absorption and bioavailability when compared to conventional herbal extract.Objective:This paper deals with the preparation, optimization and characterization of Phytosome of plant extract and in vivo assessment of antidiabetic and antihyperlipidemic activity for improved therapeutic efficacy having sufficient stability.Methods:Preliminary distinctive strategies were utilized to get ready Phytosome and antisolvent precipitation method was chosen. The formulation was guided by a full factorial design to study the effect of Independent variable on various dependent variables and resulted in an optimised product. Response contour plots were generated for each response factor to predict a phytosomal composition that yields phytosome formulation having least particle size and maximum entrapment efficiency.Results:Mean particle size, entrapment efficiency and Span value were found to be 295 ± 0.53nm, 82.43 ± 1.65% and 0.34 ± 0.14 respectively. Zeta potential was found to be 19.35mv, indicating the formation of stable formulation. In vitro release study described that the drug release follows the Korsmeyer- Peppas kinetic model. The results proved that Phytosomes of Casuarina equisetifolia extract exhibited more antidiabetic potential and antihyperlipidemic properties as compared to crude Casuarina extract.Conclusion:Phytosomes of Casuarina equestifolia extract was successfully formulated having good entrapment efficiency and physico-chemical characterization of the optimized product, confirming the formation of stable formulation. In vivo antidiabetic activity confirmed better potential of the optimised formulation. Consequently, it has been presumed that Phytosomes of Casuarina equisetifolia extract serve as a useful novel drug delivery system and provide more therapeutic efficacy than conventional plant extracts.


Author(s):  
Dr.S.Bhagavathy Sivathanu ◽  
Shivapriya G ◽  
Shivapriya G

Liposome is a spherical vesicle which contains atleast one lipid bilayer. Liposomes are used as a novel drug carriers because of its hydrophobic and hydrophilic nature, it has many advantages in the field of medical sciences. There are some other drug carriers like dendrimers, micelles, niosomes. Out of all, liposomes are considered to be the most promising agent for drug delivery. The uniqueness of liposome is when it is used as a pharmaceutical drug, it acts as a natural receptor. Thus it acts as an antigen and binds with the antibody (cancer cell) without causing any damage to the adjacent cells. For the synthesis of liposomes, a phospholipid is required. The liposomes can be synthesized using egg yolk and chloroform. So the basic phospholipid is obtained from egg yolk. For more stability, the liposomes are prepared using popc. The present work  discuss about the effective preparation of drug loaded liposomes using popc (1- palmitoyl-2-oleoyl-sn-glycero-3- phosphocholine). POPC is an important phospholipid for biophysical experiments. Additionally chloroform is used as the solvent for the liposome preparation. The drug chosen for liposome loading is vitexin (vxn), which is an effective therapeutic agent against inflammation and cancer. The vesicular size, shape, drug entrapment efficacy, stability, electrochemical property and drug releasing property of the formulated liposomes were characterized. The results showed that the formulated liposomes are considered as the better drug carrier system and good choice for biotransformation within the cell to reach the target site such as cancer cells. Even though available treatments like chemotherapy and radiation therapy, causes damage to the surrounding cells, the alternative drug transferring system such as liposomal mediated drug transfer within the cell is considered as good choice of treatment to avoid such complications. The aim of liposome mediated  drug carrier system is to develop a method to reach the drug to the target site. After drug delivery at the target site, the liposomes are fused within the surface of the body. This is because of the pH of liposomes, which is at 7.4 and temperature is maintained at 37 oC. So, the vxn loaded liposomes are considered as the novel drug carriers for the successful targetted drug delivery.


Author(s):  
Risvana Iqubal ◽  
Vimal Mathew ◽  
Kumar M. ◽  
Najiya Nasri K. V. ◽  
Safeetha Shamsudheen ◽  
...  

The poor penetration rate of the skin as a natural barrier makes transdermal drug delivery problematic. To increase transdermal dispersion of bioactives, electrophoresis, iontophoresis, chemical permeation enhancers, microneedles, sonophoresis, and vesicular systems such as liposomes, niosomes, elastic liposomes such as ethosomes, and transferosomes have all been used. Among these, transferosomes appear to be a promising option. Transferosomes are elastomeric or deformable vesicles that were originally discovered in the early 1990s. They're novel vesicular drug carrier system composed of phospholipid, surfactant, and water that improves transdermal drug delivery. Because of their low toxicity, biodegradability, ability to encapsulate both hydrophilic and lipophilic molecules, ability to prolong the drug's existence in the systemic circulation by encapsulation in vesicles, ability to target organs and tissues, and ability to reduce drug toxicity while increasing bioavailability, these vesicles are preferred over others. These vesicles undergo deformation, changes its shape and easily penetrates through the skin pores. There are two phases in any technique for preparing transferosomes. First, a thin film is hydrated before being sonicated to the required size; next, sonicated vesicles are homogenized by extrusion through a polycarbonate membrane. Transferosomes are evaluated for its entrapment efficiency, their drug content , in-vitro drug release, degree of deformability, turbidity, surface charge and morphology. Transferosomes are said to have a number of applications like delivery of vaccines,proteins, Anti-cancer drugs,anesthetics,herbal drugs and has better patient compliance,improved bio-availability and site-specific delivery and can serve as an emerging tool for transdermal delivery of almost all drugs and bio-actives.


Author(s):  
Chandani Makvana ◽  
Satyajit Sahoo

The present study was aimed to formulate, comparatively evaluate and optimize multiple lipid drug carriers of valsartan for oral controlled release to overcome the problems associated with the drug such as bioavailability, to reduce the dosage regimen, half life and to determine the appropriateness of niosomal formulation as a drug carrier. Ether injection method was chosen for the formulation of physically and chemically stable niosomes of valsartan. The formulation and process parameters were optimized by manufacturing placebo niosomes. Than drug loaded niosome was prepared by varying the concentration of span 60. The prepared nine formulations were evaluated for various parameters. Placebo niosomes were evaluated for appearance, odour, texture, creaming volume, pH and changes after 15 days. The medicated nine formulations were evaluated for organoleptic properties (appearance/color, odour), pH, total drug content, entrapment efficiency, mean particle size and polydispersibility index, zeta potential and In-vitro drug release. All formulations were off-white in color, odourless, and fluid in nature. It was stable and did not show sedimentation. The pH was found to be in the range of 4.6-5.4. Drug content was found in the range of 89.13 to 99.52. The Entrapment efficiency was found in range of 79.05 to 98.24. The mean vesicle size of drug loaded niosomes of the different batches ranged between 2.52-3.42μm. The polydispersvity index was in the range of 0.325 to 0.420 which indicates a narrow vesicle size distribution. The values of zeta potential were in the range of -20.29 mV to -30.55 mV which indicates that niosome had sufficient charge and mobility to inhibit aggregation of vesicles. All the nine formulations shows constant drug release in controlled manner up to 24 h. Formulation V7 was considered to be the best formulation as the % drug content (99.52 ± 0.97), % entrapment efficiency (98.24 ± 1.50) and % drug release at the end of 24th h (98.55) were high for V7. The optimized formulation V7 showed higher degree of correlation coefficient (r2) 0.9805 which indicates process of constant drug release from dosage form. The present study concludes that the prepared niosome is a convenient and efficiency carrier for the delivery of antihypertensive drug. Besides this, it provided controlled delivery of drug.


2019 ◽  
Vol 16 (8) ◽  
pp. 882-891
Author(s):  
Yongjia Liu ◽  
Leilei Shi ◽  
Bangshang Zhu ◽  
Yue Su ◽  
Hui Li ◽  
...  

Background: The drug-drug self-assembly was considered as a simple and efficient approach to prepare high drug loading nano-drug carriers and present new opportunities for cancer therapeutics. The strategy of PTX amphiphiles preparation would be a possible way to solve the poor water solubility of PTX. Methods: The PTX-YSL conjugate were synthesized and characterized. The PTX-YSL nanocarriers was prepared by a simple self-assembly method. In vitro cell studies and pharmacokinetic studies were evaluated for their in vitro anti-tumor activities and blood retention time. Results: The structures of PTX-YSL conjugate were confirmed by LC-MS, 1H NMR and FTIR. The size and morphology of the PTX-YSL self-assembled nanocarriers were observed with TEM and DLS. PTX-YSL nanocarriers could facilitate cellular uptake and had low cytotoxicity. PTX-YSL nanocarriers have longer blood retention for enhancing accumulation in the tumor tissues via EPR effect. Conclusion: This drug delivery system formed by PTX-YSL conjugates constitutes a promising and effective drug carrier in cancer therapy.


2019 ◽  
Vol 9 (1) ◽  
pp. 279-285 ◽  
Author(s):  
Priyanka Chaurasiya ◽  
Eisha Ganju ◽  
Neeraj Upmanyu ◽  
Sudhir Kumar Ray ◽  
Prabhat Jain

Novel drug delivery systems are now a days is creating a new interest in development of drug deliveries. Vesicular drug delivery system is also a part of these novel drug delivery systems. TDDS is the permeability of the skin, it is permeable to small molecules, lipophilic drug and highly impermeable to the macromolecules and hydrophilic drugs. Recent approaches have resulted in design of two vesicular carriers, ethosomes and ultra flexible lipid based elastic vesicles, transferosomes. Transferosomes have recently been introduced, which are capable of transdermal delivery of low as well as high molecular weight drugs. This offers several potential advantages over conventional routes like avoidance of first pass metabolism, predictable and extended duration of activity, minimizing undesirable side effects, utility of short half life drugs, improving physiological and pharmacological response and have been applied to increases the efficiency of the material transfer across the intact skin, by the use of penetration enhancers, iontophoresis, sonophoresis and use of colloidal carriers such as lipid vesicles (liposomes & proliposomes) and non-ionic surfactant vesicles (niosomes & proniosomes). It is suitable for controlled and targeted drug delivery and it can accommodate drug molecules with wide range of solubility. Due to its high deformability it gives better penetration of intact vesicles. They are biocompatible and biodegradable as they are made from natural phospholipids and have high entrapment efficiency. The preparation variables are depending upon the procedure involved for manufacturing of formulation and the preparation procedure was accordingly optimized and validated. Characterization of transferosomes can be done to know the vesicle size, morphology, drug content, entrapment efficiency, penetration ability, occlusion effect, surface charge, in vitro drug release, in vitro skin penetration etc., It increases stability of labile drugs and provides control release. Transferosomes thus differs from such more conventional vesicles primarily by its softer, more deformable, better adjustable artificial membrane. Keywords: Novel Drug Delivery System, Biocompatible, Characterization, Transferosomes.


2021 ◽  
Vol 2 (1) ◽  
pp. 116-126
Author(s):  
Neha Rani ◽  
Rupali Rana ◽  
Reena Thakur ◽  
Shivali Singla ◽  
Sachin Goyal

Atorvastatin calcium is a HMG-CoA reductase inhibitor used for the treatment of hyperlipidaemia. It has oral bioavailability of ≤12 %. It also undergoes high first pass metabolism. It is highly soluble in acidic pH and absorbed more in the upper part of the gastrointestinal tract. In order, to improve the absorption and its oral bioavailability, niosomes of Atorvastatin calcium have been formulated and evaluated on different parameters. Niosomes play an increasingly important role in drug delivery as they can reduce toxicity and 000000000modify pharmacokinetic and bio-availability. Niosomes formulations of Atorvastatin calcium were successfully developed by thin film hydration technique using nonionic surfactant i.e. Span 40, Span 60 Span 80, Tween 20, Tween 40, Tween 80 and cholesterol at different concentrations. The formulations were evaluated for size, shape, and entrapment efficiency. In-vitro release and stability studies also performed. Results indicated that Niosomes were prepared succesfully work as promising drug carriers and promising drug delivery module.


Author(s):  
G D Chandrethiya ◽  
P K Shelat ◽  
M N Zaveri

PEGylated gelatin nanoparticles loaded with colchicine were prepared by ethanol precipitation method. Poly-(ethylene glycol)-5000-monomethylether (MPEG 5000), a hydrophilic polymer, was used to pegylate gelatin.  Gluteraldehyde was used as cross-linking agent. To obtain a high quality product, major formulation parameters were optimized.  Spherical particles with mean particles of 193 nm were measured by a Malvern particle size analyzer. Entrapment efficiency was found to be 71.7 ± 1.4% and determined with reverse phase high performance liquid charomatography (RP-HPLC). The in vitro drug release study was performed by dialysis bag method for a period of 168 hours. Lyophilizaton study showed sucrose at lower concentrations proved the best cryoprotectant for this formulation.  Stability study revealed that lyophilized nanoparticles were equally effective (p < 0.05) after one year of storage at 2-8°C with ambient humidity. In vitro antitumoral activity was accessed using the MCF-7 cell line by MTT assay.  The IC50 value was found to be 0.034 μg/ml for the prepared formulation. The results indicate that PEGylated gelatin nanoparticles could be utilized as a potential drug delivery for targeted drug delivery of tumors.  


Author(s):  
J M Shah ◽  
N.H Shah ◽  
Hadiya P D

Pharmaceutical technology has developed various newer modes of novel drug delivery aspects. Modifications in the previously existing drug delivery methods have led to various newly innovated technologies serving as a safe and effective means of improvement over the existing ones. Novasome technology is one of the new innovations of liposomes which have solved many of the problems related to liposomal drug delivery system. It offers a seven bilayer membrane which has the ability to incorporate both water soluble and insoluble drugs. It has an excellent entrapment efficiency which provides better medication. Formulation of novasomes is achieved in a high shear device. Due to its numerous advantages, novasomes have been used extensively in various fields like cosmetics, chemical, personal care, foods, pharmaceuticals and agrochemicals.


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