Oil-Cyclodextrin Based Beads for Oral Delivery of Poorly-Soluble Drugs

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.

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

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2011.12.010 ◽

2012 ◽

Vol 423 (2) ◽

pp. 452-460 ◽

Cited By ~ 33

Author(s):

Nicolas Duhem ◽

Julien Rolland ◽

Raphaël Riva ◽

Pierre Guillet ◽

Jean-Marc Schumers ◽

...

Keyword(s):

Oral Delivery ◽

Poorly Soluble Drugs ◽

Glycol Chitosan ◽

Poorly Soluble

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

Molecular Pharmaceutics ◽

10.1021/mp900221e ◽

2009 ◽

Vol 7 (1) ◽

pp. 227-236 ◽

Cited By ~ 109

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

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Improved Oral Delivery of Drugs Using Nanoemulsion

10.4018/978-1-7998-8378-4.ch005 ◽

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.

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