Novel nanostructured lipid carrier for oral delivery of a poorly soluble antimalarial agent lumefantrine: characterization and pharmacokinetics evaluation

2018 ◽  
Vol 5 (1) ◽  
Author(s):  
Guihua Huang ◽  
Jingjing Liu ◽  
Liu Tian ◽  
Shilei Chen
Keyword(s):  
Oral Delivery ◽  
Nanostructured Lipid Carrier ◽  
Antimalarial Agent ◽  
Poorly Soluble

scholarly journals Relative Contributions of Solubility and Mobility to the Stability of Amorphous Solid Dispersions of Poorly Soluble Drugs: A Molecular Dynamics Simulation Study

Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 101 ◽  
Author(s):  
Michael Brunsteiner ◽  
Johannes Khinast ◽  
Amrit Paudel
Keyword(s):  
Molecular Dynamics ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Dynamics Simulation ◽  
Limiting Factor ◽  
Poorly Soluble Drugs ◽  
Formulation Development ◽  
Amorphous Solid Dispersions ◽  
Poorly Soluble

Amorphous solid dispersions are considered a promising formulation strategy for the oral delivery of poorly soluble drugs. The limiting factor for the applicability of this approach is the physical (in)stability of the amorphous phase in solid samples. Minimizing the risk of reduced shelf life for a new drug by establishing a suitable excipient/polymer-type from first principles would be desirable to accelerate formulation development. Here, we perform Molecular Dynamics simulations to determine properties of blends of eight different polymer–small molecule drug combinations for which stability data are available from a consistent set of literature data. We calculate thermodynamic factors (mixing energies) as well as mobilities (diffusion rates and roto-vibrational fluctuations). We find that either of the two factors, mobility and energetics, can determine the relative stability of the amorphous form for a given drug. Which factor is rate limiting depends on physico-chemical properties of the drug and the excipients/polymers. The methods outlined here can be readily employed for an in silico pre-screening of different excipients for a given drug to establish a qualitative ranking of the expected relative stabilities, thereby accelerating and streamlining formulation development.

scholarly journals High-Throughput Excipient Discovery Enables Oral Delivery of Poorly Soluble Pharmaceuticals

2016 ◽  
Vol 2 (10) ◽  
pp. 748-755 ◽  
Author(s):  
Jeffrey M. Ting ◽  
Swapnil Tale ◽  
Anatolii A. Purchel ◽  
Seamus D. Jones ◽  
Lakmini Widanapathirana ◽  
...  
Keyword(s):  
High Throughput ◽  
Oral Delivery ◽  
Poorly Soluble

Tocol modified glycol chitosan for the oral delivery of poorly soluble drugs

2012 ◽  
Vol 423 (2) ◽  
pp. 452-460 ◽  
Author(s):  
Nicolas Duhem ◽  
Julien Rolland ◽  
Raphaël Riva ◽  
Pierre Guillet ◽  
Jean-Marc Schumers ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Poorly Soluble Drugs ◽  
Glycol Chitosan ◽  
Poorly Soluble

Oxidized Mesoporous Silicon Microparticles for Improved Oral Delivery of Poorly Soluble Drugs

2009 ◽  
Vol 7 (1) ◽  
pp. 227-236 ◽  
Author(s):  
Feng Wang ◽  
He Hui ◽  
Timothy J. Barnes ◽  
Christian Barnett ◽  
Clive A. Prestidge
Keyword(s):  
Oral Delivery ◽  
Poorly Soluble Drugs ◽  
Mesoporous Silicon ◽  
Poorly Soluble

Improved Oral Delivery of Drugs Using Nanoemulsion

2022 ◽  
pp. 93-117
Author(s):  
Subramanian Natesan ◽  
Victor Hmingthansanga ◽  
Nidhi Singh ◽  
Pallab Datta ◽  
Sivakumar Manickam ◽  
...  
Keyword(s):  
Oral Administration ◽  
Oral Delivery ◽  
Oral Route ◽  
Poorly Soluble Drugs ◽  
Site Specific ◽  
Anatomy And Physiology ◽  
Oral Application ◽  
Biological Fate ◽  
Poorly Soluble ◽  
Low Solubility

Administration of drugs through the oral route is considered the simplest and most convenient way to offer greater patient compliance than other routes. Most active drugs discovered in the past and those being discovered in recent times are inadequate because of their inherent limitations in physicochemical properties such as low solubility and permeability, resulting in poor bioavailability, especially after oral administration in the form of tablet or capsule. Pharmaceutical nanoemulsion is the most promising, safer, and multimodal technique for delivering poorly soluble drugs and gaining more attention due to its characteristics such as higher solubilisation capacity, smaller size, surface charge, and site-specific drug targeting. This chapter focuses on the biological fate of nanoemulsion after oral administration and a few case studies related to the oral application of nanoemulsion in delivering poorly soluble drugs. In addition, the anatomy and physiology of the GI tract, components of nanoemulsion, and methods of preparation are addressed.

Chapter 5 Oral Delivery of Poorly Soluble Drugs

2017 ◽  
pp. 125-186
Author(s):  
Dev Prasad ◽  
Akash Jain ◽  
Sudhakar Garad
Keyword(s):  
Oral Delivery ◽  
Poorly Soluble Drugs ◽  
Poorly Soluble

scholarly journals β-Sitosterol Loaded Nanostructured Lipid Carrier: Physical and Oxidative Stability, In Vitro Simulated Digestion and Hypocholesterolemic Activity

Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 386
Author(s):  
Yasamin Soleimanian ◽  
Sayed Amir Hossein Goli ◽  
Jaleh Varshosaz ◽  
Lorenzo Di Cesare Mannelli ◽  
Carla Ghelardini ◽  
...  
Keyword(s):  
Oxidative Stability ◽  
Oral Delivery ◽  
Physical Stability ◽  
Density Lipoprotein ◽  
Water Soluble ◽  
Nanostructured Lipid Carrier ◽  
Lipid Mixture ◽  
Simulated Digestion

The objective of the present study was to explore the potential of nanostructured lipid carriers (NLCs) for improving the oral delivery of β-sitosterol, a poorly water-soluble bioactive component with hypocholesterolemic activity. Two β-sitosterol formulations with different solid lipid compositions were prepared by melt emulsification, followed by the sonication technique, and the effect of storage conditions and simulated digestion on the physical, chemical and oxidative stability, bioaccessibility and release were extensively studied. Both NLC preparations remained relatively stable during the four weeks of storage at different conditions (4, 25 and 40 °C), with more superior stability at lower temperatures. The in vitro digestion experiment indicated a high physical stability after exposure to the simulated mouth and stomach stages and an improved overall β-sitosterol bioaccessibility at the end of the digestion. The NLCs presented an increased solubility and gradual release which could be justified by the remarkable affinity of β-sitosterol to the complex lipid mixture. An in vivo study demonstrated an improved reduction in the total cholesterol and low-density lipoprotein cholesterol plasma levels in mice compared with the drug suspension. These investigations evidenced the potential of the developed NLC formulations for the enhancement of solubility and in vivo performance of β-sitosterol.

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