scholarly journals Buparvaquone Nanostructured Lipid Carrier: Development of an Affordable Delivery System for the Treatment of Leishmaniases

2017 ◽  
Vol 2017 ◽  
pp. 1-11 ◽  
Author(s):  
Lis Marie Monteiro ◽  
Raimar Löbenberg ◽  
Paulo Cesar Cotrim ◽  
Gabriel Lima Barros de Araujo ◽  
Nádia Bou-Chacra
Keyword(s):  
Drug Delivery ◽  
Delivery System ◽  
Design Space ◽  
Water Solubility ◽  
Raw Materials ◽  
Low Cost ◽  
Scale Up ◽  
Veterinary Drug ◽  
Nanostructured Lipid Carrier ◽  
The Relationship

Buparvaquone (BPQ), a veterinary drug, was formulated as nanostructured lipid carriers (NLC) for leishmaniases treatment. The formulation design addressed poor water solubility of BPQ and lack of human drug delivery system. The DSC/TG and microscopy methods were used for solid lipids screening. Softisan® 154 showed highest BPQ solubility in both methods. The BPQ solubility in liquid lipids using HPLC revealed Miglyol® 812 as the best option. Response surface methodology (RSM) was used to identify the optimal Softisan154 : Miglyol 812 ratios (7 : 10 to 2 : 1) and Kolliphor® P188 and Tween® 80 concentration (>3.0% w/w) aiming forz-average in the range of 100–300 nm for macrophage delivery. The NLC obtained by high-pressure homogenization showed lowz-averages (<350 nm), polydispersity (<0.3), and encapsulation efficiency close to 100%. DSC/TG and microscopy in combination proved to be a powerful tool to select the solid lipid. The relationship among the variables, demonstrated by a linear mathematical model using RSM, allowed generating a design space. This design space showed the limits in which changes in the variables influenced thez-average. Therefore, these drug delivery systems have the potential to improve the availability of affordable medicines due to the low cost of raw materials, using well established, reliable, and feasible scale-up technology.

An Overview of Second Generation Nanoparticles− Nanostructure Lipid Carrier Drug Delivery System

2020 ◽  
Vol 13 (6) ◽  
pp. 5181-5189
Author(s):  
Prabhat Kumar Sahoo ◽  
Neha S.L ◽  
Arzoo Pannu
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Second Generation ◽  
Drug Loading ◽  
Scale Up ◽  
Delivery Systems ◽  
Route Of Administration ◽  
Random Structure ◽  
Stability Parameters

Lipids are used as vehicles for the preparation of various formulations prescribed for administrations, including emulsions, ointments, suspension, tablets, and suppositories. The first parental nano-emulsion was discovered from the 1950s when it was added to the intravenous administration of lipid and lipid-soluble substances. Lipid-based drug delivery systems are important nowadays. Solid nanoparticles (SLN) and Nanostructured lipid carriers (NLC) are very proficient due to the ease of production process, scale-up capability, bio-compatibility, the biodegradability of formulation components and other specific features of the proposed route. The administration or nature of the materials must be loaded into these delivery systems. The main objectives of this review are to discuss an overview of second-generation nanoparticles, their limitations, structures, and route of administration, with emphasis on the effectiveness of such formulations. NLC is the second generation of lipid nanoparticles having a structure like nanoemulsion. The first generation of nanoparticles was SLN. The difference between both of them is at its core. Both of them are a colloidal carrier in submicron size in the range of 40-1000 nm. NLC is the most promising novel drug delivery system over the SLN due to solving the problem of drug loading and drug crystallinity. Solid and liquid lipids combination in NLC formation, improve its quality as compare to SLN. NLC has three types of structures: random, amorphous, and multiple. The random structure containing solid-liquid lipids and consisting crystal and the liquid lipid irregular in shape; thereby enhance the ability of the lipid layer to pass through the membrane. The second is the amorphous structure. It is less crystalline in nature and can prevent the leakage of the loaded drug. The third type is multiple structures, which have higher liquid lipid concentrations than other types. The excipients used to form the NLC are bio-compatible, biodegradable and non-irritating, most of which can be detected using GRAS. NLC is a promising delivery system to deliver the drug through pulmonary, ocular, CNS, and oral route of administration. Various methods of preparation and composition of NLC influence its stability Parameters. In recent years at the educational level, the potential of NLC as a delivery mechanism targeting various organs has been investigated in detail.

scholarly journals Recent Findings in Azaphilone Pigments

2021 ◽  
Vol 7 (7) ◽  
pp. 541
Author(s):  
Lúcia P. S. Pimenta ◽  
Dhionne C. Gomes ◽  
Patrícia G. Cardoso ◽  
Jacqueline A. Takahashi
Keyword(s):  
Water Solubility ◽  
Biological Activities ◽  
Low Cost ◽  
Scale Up ◽  
Structural Diversity ◽  
Downstream Processing ◽  
Global Market ◽  
Yield Improvement ◽  
Potential Applications ◽  
New Compounds

Filamentous fungi are known to biosynthesize an extraordinary range of azaphilones pigments with structural diversity and advantages over vegetal-derived colored natural products such agile and simple cultivation in the lab, acceptance of low-cost substrates, speed yield improvement, and ease of downstream processing. Modern genetic engineering allows industrial production, providing pigments with higher thermostability, water-solubility, and promising bioactivities combined with ecological functions. This review, covering the literature from 2020 onwards, focuses on the state-of-the-art of azaphilone dyes, the global market scenario, new compounds isolated in the period with respective biological activities, and biosynthetic pathways. Furthermore, we discussed the innovations of azaphilone cultivation and extraction techniques, as well as in yield improvement and scale-up. Potential applications in the food, cosmetic, pharmaceutical, and textile industries were also explored.

A Review on Formulation and Development of Solid Self-Nano Emulsifying Drug Delivery Systems

2021 ◽  
Vol 14 (4) ◽  
pp. 5519-5228
Author(s):  
Sunitha M Reddy ◽  
Sravani Baskarla
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Drug Loading ◽  
Aqueous Solubility ◽  
Delivery Systems ◽  
Particle Size Reduction

This article describes current strategies to enhance aqueous solubility and dissolution rate of poor soluble drugs. Most drugs in the market are lipophilic with low or poor water solubility. There are various methods to enhance solubility: co-solvency, particle size reduction, salt formation and Self Nanoemulsifying drug delivery systems, SEDDS is a novel approach to enhance solubility, dissolution rate and bioavailability of drugs. The study involves formulation and evaluation of solid self-Nano emulsifying drug delivery system (S-SNEDDS) to enhance aqueous solubility and dissolution rate. Oral route is the most convenient route for non-invasive administration. S-SNEDDS has more advantages when compared to the liquid self-emulsifying drug delivery system. Excipients were selected depends upon the drug compatibility oils, surfactants and co surfactants were selected to formulate Liquid SNEDDS these formulated liquid self-nano emulsifying drug delivery system converted into solid by the help of porous carriers, Melted binder or with the help of drying process. Conversion process of liquid to solid involves various techniques; they are spray drying; freeze drying and fluid bed coating technique; extrusion, melting granulation technique. Liquid SNEDDS has a high ability to improve dissolution and solubility of drugs but it also has disadvantages like incompatibility, decreased drug loading, shorter shelf life, ease of manufacturing and ability to deliver peptides that are prone to enzymatic hydrolysis.  

scholarly journals Synthesis, Characterization, and Evaluation of a Novel Amphiphilic Polymer RGD-PEG-Chol for Target Drug Delivery System

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Shi Zeng ◽  
Fengbo Wu ◽  
Bo Li ◽  
Xiangrong Song ◽  
Yu Zheng ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Large Scale ◽  
Film Formation ◽  
Low Cost ◽  
Amphiphilic Polymer ◽  
Target Drug Delivery ◽  
H Nmr ◽  
Target Drug

An amphiphilic polymer RGD-PEG-Chol which can be produced in large scale at a very low cost has been synthesized successfully. The synthesized intermediates and final products were characterized and confirmed by1H nuclear magnetic resonance spectrum (1H NMR) and Fourier transform infrared spectrum (FT-IR). The paclitaxel- (PTX-) loaded liposomes based on RGD-PEG-Chol were then prepared by film formation method. The liposomes had a size within 100 nm and significantly enhanced the cytotoxicity of paclitaxel to B16F10 cell as demonstrated by MTT test (IC50= 0.079 μg/mL of RGD-modified PTX-loaded liposomes compared to 9.57 μg/mL of free PTX). Flow cytometry analysis revealed that the cellular uptake of coumarin encapsulated in the RGD-PEG-Chol modified liposome was increased for HUVEC cells. This work provides a reasonable, facile, and economic approach to prepare peptide-modified liposome materials with controllable performances and the obtained linear RGD-modified PTX-loaded liposomes might be attractive as a drug delivery system.

scholarly journals Niosomes: Potential Nanocarriers for Drug Delivery

2020 ◽  
Vol 11 (03) ◽  
pp. 389-394
Author(s):  
Ashish Suttee ◽  
Vijay Mishra ◽  
Pallavi Nayak ◽  
Manvendra Singh ◽  
Pavani Sriram
Keyword(s):  
Drug Delivery ◽  
Delivery System ◽  
Scale Up ◽  
Production Costs ◽  
Ionic Surfactant ◽  
Drug Bioavailability ◽  
Pharmacological Agents ◽  
Drug Degradation ◽  
Advantages And Disadvantages ◽  
Traditional Drug

Niosomes are novel vesicular drug delivery systems, where the solution is surrounded by non-ionic surfactant vesicles. The niosomes offer different benefits over the traditional drug delivery system. Niosomes are structurally similar to liposomes, as they also consist of a bilayer. In the case of niosomes, the bilayer consists of non-ionic surface-active agents instead of phospholipids, as seen in liposomes. Niosomes are much more stable during the process of formulation and storage, as compared to liposomes. Niosomes may resolve the issues of insolubility, volatility, poor bioavailability, and rapid drug degradation. It has been discovered in recent years that, these vesicles can enhance drug bioavailability and can act as a new strategy to deliver many conventional therapeutic agents, such as, protein drugs, and gene materials. It is also easy to prepare and scale up this novel delivery system with low production costs. The delivery of drugs via niosomal formulations may be relevant to several pharmacological agents for their activity against different diseases. The present review provides an overview about the advantages and disadvantages, fabrication techniques, types, characterization technique, and different applications of niosomes.

scholarly journals A Literature Review on Self Nanoemulsifying Drug Delivery System (SNEDDS)

2021 ◽  
Vol 70 (1) ◽  
Author(s):  
Saikumar D ◽  
Leela Prasanna J
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Water Solubility ◽  
Solvent Molecule ◽  
Water Soluble ◽  
Statistical Experimental Design ◽  
Characterization Methods ◽  
Nano Emulsion ◽  
Pharmacologically Active

The Lipid-based drug delivery system is extensively reported within the literature for the enhancing drug solubility, permeability, and bioavailability. A considerable majority of novel pharmacologically active constituents produced in recent drug discovery programs are lipophilic and poorly soluble, posing a significant problem for pharmaceutical researchers enhancing the oral bioavailability of such drug molecules. Self-nano emulsifying drug delivery systems (SNEDDS), are the viable oil-based approaches for drugs that exhibit low dissolution rate and inadequate absorption. Ever since the progress of SNEDDS, researchers have been focusing on the challenges of BCS Class II and Class IV Drugs for enhancing water Solubility of poorly water-soluble drugs. SNEDDS is a Validate method for enhancing the solubility and bioavailability of lipophilic compounds. It’s the isotropic mixture of oil, surfactant, co-surfactant molecules and it also containing co-solvent molecule. which spontaneously form oil-in-water nano emulsion of approximately 200 nm or less in size upon dilution with water under gentle stirring. It’s Drug delivery system Which possess thermodynamically and kinetically stability. The physicochemical properties, drug solubilization capacity considerably regulates the selection of the SNEDDS components. The compositions of the SNEDDS are often optimized with the assistance of phase diagrams. Further to optimize SNEDDS can be done with the help of statistical experimental design. It’s a Novel drug delivery system which is applicable for the parenteral, Ophthalmic, intranasal and cosmetic drug delivery system. And therefore, the present review describes Preparation, components, mechanism of self-Nano emulsification, biopharmaceutical aspects, characterization methods and applications of Selfnanoemulsifying drug delivery system (SNEDDS).

Quaternized Chitosan Modified Nanostructure Lipid Carriers for Topical Delivery of Coenzyme Q10

Nano LIFE ◽  
2020 ◽  
Vol 10 (04) ◽  
pp. 2040013 ◽  
Author(s):  
Rong Liang ◽  
Yuxuan Wang ◽  
Lina Wu ◽  
Xinjiong Ni ◽  
Cheng Yang
Keyword(s):  
Delivery System ◽  
Coenzyme Q10 ◽  
Transdermal Delivery ◽  
Laser Scanning ◽  
Water Solubility ◽  
Laser Scanning Microscopy ◽  
Confocal Laser ◽  
Nanostructured Lipid Carrier ◽  
Quaternized Chitosan

Nanostructured lipid carrier (NLC) is a new colloidal delivery system which can effectively solve the problems of stability and transdermal delivery of active ingredients with poor water solubility and biocompatibility. Coenzyme Q10 (CoQ10), as a lipophilic antioxidant, has poor chemical stability due to unsaturated double bonds in its molecular structure, which limits its addition and application in cosmetics. In this study, CoQ10 NLC was prepared using the mixture of Caprylyl/Capryl Glycoside (APG) and quaternized chitosan (QCS). The particle size of the QCS–APG–NLC was around 250 nm. Compared to NLC stabilized by APG, QCS–APG–NLC has better storage stability under high temperature and light conditions. In vitro transdermal experiment analysis and confocal laser scanning microscopy (CLSM) observation found that QCS modification can effectively increase the penetration amount of CoQ10 in the skin. So, it is suggested that QCS modified APG–NLC can be used as an effective transdermal delivery system for lipophilic active components.

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