scholarly journals TheIn VitroLipolysis of Lipid-Based Drug Delivery Systems: A Newly Identified Relationship between Drug Release and Liquid Crystalline Phase

2016 ◽  
Vol 2016 ◽  
pp. 1-9
Author(s):  
Lu Xiao ◽  
Tao Yi ◽  
Ying Liu ◽  
Hua Zhou
Keyword(s):  
Drug Delivery ◽  
Crystalline Phase ◽  
Drug Delivery Systems ◽  
Liquid Crystalline ◽  
Delivery Systems ◽  
Liquid Crystalline Phase ◽  
Type I ◽  
Type Ii ◽  
Type Iv

The purpose of this study was to offer a new insight into the microstructure changes duringin vitrolipolysis of five lipid-based drug delivery formulations belonging to different lipid formulation types. Five lipid-based formulations of indomethacin were investigated using anin vitrolipolysis model. During lipolysis, microstructures of the intermediate phase formed by lipolytic products were observed. The results showed that the time of liquid crystal formation duringin vitrodigestion for these formulations was Type I > Type II > Type IIIB > Type IV > Type IIIA (p<0.05). After lipolysis, the drug releases from these formulations were determined. The results showed that the amount of drug distributed in the aqueous phase, obtained by ultracentrifuge after lipolysis, was, astonishingly, in inverse rank order of the above mentioned, that is, Type IIIA > Type IV > Type IIIB > Type II > Type I (p<0.05). These results showed that the liquid crystalline phase probably has a critical influence on the fate of the drug duringin vitrolipolysis and suggested that the liquid crystalline phase facilitated drug precipitation. These findings may improve the understanding of lipolysis of lipid-based drug delivery systems for designing better delivery system.

scholarly journals Synthesis, characterization and bioevaluation of irinotecan-collagen hybrid materials for biomedical applications as drug delivery systems in tumoral treatments

2013 ◽  
Vol 11 (12) ◽  
pp. 2134-2143 ◽  
Author(s):  
Georgeta Voicu ◽  
Ruxandra Geanaliu ◽  
Cristina Ghiţulică ◽  
Anton Ficai ◽  
Alexandru Grumezescu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Hybrid Materials ◽  
Biomedical Applications ◽  
Drug Delivery Systems ◽  
Local Treatment ◽  
Collagen Type I ◽  
Delivery Systems ◽  
Antitumoral Activity ◽  
Type I

AbstractThe purpose of the present study is the preparation and characterization of collagen/antitumor drug hybrids as drug delivery systems. Materials used for obtaining collagen-based drug delivery systems were collagen type I (Coll) as matrix and irinotecan (I) as hydrophilic active substances. After incorporation of I into Coll in differing ratios, the obtained hybrid materials (Coll/I) could be used according to our results as potential drug delivery systems in medicine for the topical (local) treatment of cancerous tissues or bone. The released amount of I varies with amount of Coll from hybrid materials: the higher, the slower the release amount of irinotecan transferred is in the first 6 hours. The in vitro citotoxicity demonstrates an antitumoral activity of the obtained hybrid materials and their potential use for biomedical applications as drug delivery systems in tumoral treatments.

Self-Emulsifying Delivery Systems for Poorly Absorbed Drugs

1970 ◽  
Vol 1 (2) ◽  
pp. 123-128
Author(s):  
Jayvadan Patel ◽  
Anand Shah
Keyword(s):  
Drug Delivery ◽  
Crystalline Phase ◽  
Oral Bioavailability ◽  
Energy Input ◽  
Drug Delivery Systems ◽  
Liquid Crystalline ◽  
Delivery Systems ◽  
Water Interface ◽  
Oil Water ◽  
Emulsification Process

Self-emulsifying drug delivery systems (SEDDS) are a type of emulsion that have received particular attention in recent years as a means of enhancing oral bioavailability of poorly absorbed drugs. These systems are ideally isotropic mixture of oil and surfactant (sometimes co-surfactant are added) that form emulsions on mixing with water with little or no energy input. Hydrophobic drugs are dissolved in SEDDS. After administering the drug by this system, emulsion is formed in the GIT by selfemulsification. Generally by this process bioavailability of the drug is increased and quantity required to exert desired effect is decreased. Oil surfactant ratio, amount of surfactant, type of surfactant, nature of oil affect the process of emulsification. In the emulsification process water penetrates into the oil water interface, leading to the formation of liquid crystalline phase, resulting in swelling at the interface. Generally, SEDDS are formed with triglyceride oils and nonionic surfactant. In the GIT, during the digestion of fat, drugs are getting released and lead to increase the absorption of drug by dissolution or by particle charges which increase the bioavailability. Some latest related to SEDDS is described in this review.

scholarly journals In-Silico Screening of Lipid-Based Drug Delivery Systems

2020 ◽  
Vol 37 (12) ◽  
Author(s):  
Joscha Brinkmann ◽  
Lara Exner ◽  
Christian Luebbert ◽  
Gabriele Sadowski
Keyword(s):  
Drug Delivery ◽  
In Silico ◽  
Drug Delivery Systems ◽  
Screening Method ◽  
Delivery Systems ◽  
Type I ◽  
In Silico Screening ◽  
Statistical Associating Fluid Theory ◽  
Type Iv ◽  
Type Iiib

Abstract Purpose This work proposes an in-silico screening method for identifying promising formulation candidates in complex lipid-based drug delivery systems (LBDDS). Method The approach is based on a minimum amount of experimental data for API solubilites in single excipients. Intermolecular interactions between APIs and excipients as well as between different excipients were accounted for by the Perturbed-Chain Statistical Associating Fluid Theory. The approach was applied to the in-silico screening of lipid-based formulations for ten model APIs (fenofibrate, ibuprofen, praziquantel, carbamazepine, cinnarizine, felodipine, naproxen, indomethacin, griseofulvin and glibenclamide) in mixtures of up to three out of nine excipients (tricaprylin, Capmul MCM, caprylic acid, Capryol™ 90, Lauroglycol™ FCC, Kolliphor TPGS, polyethylene glycol, carbitol and ethanol). Results For eight out of the ten investigated model APIs, the solubilities in the final formulations could be enhanced by up to 100 times compared to the solubility in pure tricaprylin. Fenofibrate, ibuprofen, praziquantel, carbamazepine are recommended as type I formulations, whereas cinnarizine and felodipine showed a distinctive solubility gain in type II formulations. Increased solubility was found for naproxen and indomethacin in type IIIb and type IV formulations. The solubility of griseofulvin and glibenclamide could be slightly enhanced in type IIIb formulations. The experimental validation agreed very well with the screening results. Conclusion The API solubility individually depends on the choice of excipients. The proposed in-silico-screening approach allows formulators to quickly determine most-appropriate types of lipid-based formulations for a given API with low experimental effort. Graphical abstract

scholarly journals Skin Delivery of Kojic Acid-Loaded Nanotechnology-Based Drug Delivery Systems for the Treatment of Skin Aging

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
M. L. Gonçalez ◽  
M. A. Corrêa ◽  
M. Chorilli
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Liquid Crystalline ◽  
Kojic Acid ◽  
Skin Permeation ◽  
Polarized Light ◽  
Skin Aging ◽  
Delivery Systems ◽  
Skin Delivery

The aging process causes a number of changes in the skin, including oxidative stress and dyschromia. The kojic acid (KA) is iron chelator employed in treatment of skin aging, and inhibits tyrosinase, promotes depigmentation. Nanotechnology-based drug delivery systems, such as liquid crystalline systems (LCSs), can modulate drug permeation through the skin and improve the drug activity. This study is aimed at structurally developing and characterizing a kojic acid-loaded LCS, consists of water (W), cetostearyl isononanoate (oil—O) and PPG-5-CETETH-20 (surfactant-S) and evaluating itsin vitroskin permeation and retention. Three regions of the diagram were selected for characterization: A (35% O, 50% S, 15% W), B (30% O, 50% S, 20% W) and C (20% O, 50% S, 30% W), to which 2% KA was added. The formulations were subjected to polarized light microscopy, which indicated the presence of a hexagonal mesophase. Texture and bioadhesion assay showed that formulation B is suitable for topical application. According to the results from thein vitropermeation and retention of KA, the formulations developed can modulate the permeation of KA in the skin. Thein vitrocytotoxic assays showed that KA-unloaded LCS and KA-loaded LCS didn't present cytotoxicity. PPG-5-CETETH-20-based systems may be a promising platform for KA skin delivery.

scholarly journals Advanced Static and Dynamic Fluorescence Microscopy Techniques to Investigate Drug Delivery Systems

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 861
Author(s):  
Jacopo Cardellini ◽  
Arianna Balestri ◽  
Costanza Montis ◽  
Debora Berti
Keyword(s):  
Drug Delivery ◽  
Fluorescence Microscopy ◽  
Drug Delivery Systems ◽  
Laser Scanning ◽  
Super Resolution ◽  
Laser Scanning Confocal Microscopy ◽  
Delivery Systems ◽  
Scanning Confocal Microscopy ◽  
Biological Phenomena

In the past decade(s), fluorescence microscopy and laser scanning confocal microscopy (LSCM) have been widely employed to investigate biological and biomimetic systems for pharmaceutical applications, to determine the localization of drugs in tissues or entire organisms or the extent of their cellular uptake (in vitro). However, the diffraction limit of light, which limits the resolution to hundreds of nanometers, has for long time restricted the extent and quality of information and insight achievable through these techniques. The advent of super-resolution microscopic techniques, recognized with the 2014 Nobel prize in Chemistry, revolutionized the field thanks to the possibility to achieve nanometric resolution, i.e., the typical scale length of chemical and biological phenomena. Since then, fluorescence microscopy-related techniques have acquired renewed interest for the scientific community, both from the perspective of instrument/techniques development and from the perspective of the advanced scientific applications. In this contribution we will review the application of these techniques to the field of drug delivery, discussing how the latest advancements of static and dynamic methodologies have tremendously expanded the experimental opportunities for the characterization of drug delivery systems and for the understanding of their behaviour in biologically relevant environments.

scholarly journals Mechanisms and Pharmaceutical Action of Lipid Nanoformulation of Natural Bioactive Compounds as Efficient Delivery Systems in the Therapy of Osteoarthritis

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1108
Author(s):  
Oana Craciunescu ◽  
Madalina Icriverzi ◽  
Paula Ecaterina Florian ◽  
Anca Roseanu ◽  
Mihaela Trif
Keyword(s):  
Drug Delivery ◽  
Bioactive Compounds ◽  
Targeted Delivery ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Joint Disease ◽  
Duration Of Action ◽  
Immune System Activation

Osteoarthritis (OA) is a degenerative joint disease. An objective of the nanomedicine and drug delivery systems field is to design suitable pharmaceutical nanocarriers with controllable properties for drug delivery and site-specific targeting, in order to achieve greater efficacy and minimal toxicity, compared to the conventional drugs. The aim of this review is to present recent data on natural bioactive compounds with anti-inflammatory properties and efficacy in the treatment of OA, their formulation in lipid nanostructured carriers, mainly liposomes, as controlled release systems and the possibility to be intra-articularly (IA) administered. The literature regarding glycosaminoglycans, proteins, polyphenols and their ability to modify the cell response and mechanisms of action in different models of inflammation are reviewed. The advantages and limits of using lipid nanoformulations as drug delivery systems in OA treatment and the suitable route of administration are also discussed. Liposomes containing glycosaminoglycans presented good biocompatibility, lack of immune system activation, targeted delivery of bioactive compounds to the site of action, protection and efficiency of the encapsulated material, and prolonged duration of action, being highly recommended as controlled delivery systems in OA therapy through IA administration. Lipid nanoformulations of polyphenols were tested both in vivo and in vitro models that mimic OA conditions after IA or other routes of administration, recommending their clinical application.

Sign in / Sign up

Export Citation Format

Share Document