Improved Oral Delivery of Drugs Using Nanoemulsion

2022 ◽  
pp. 93-117
Author(s):  
Subramanian Natesan ◽  
Victor Hmingthansanga ◽  
Nidhi Singh ◽  
Pallab Datta ◽  
Sivakumar Manickam ◽  
...  

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.

2021 ◽  
Vol 11 (1-s) ◽  
pp. 200-206
Author(s):  
Ashwin Bhanudas Kuchekar ◽  
Ashwini Gawade ◽  
Sanjay Boldhane

Drug development plays an important role in patient safety and effectiveness. The therapeutic suitability of a new drug depends on the solubility. The solubility of the sparingly soluble drug remains a problem in identifying new active compounds. Solubility plays an important role in achieving optimal drug concentration. Low solubility is not only a concern for the production of formulations, but also an obstacle from the outset when identifying active chemicals for therapeutic purposes. Due to its simplicity in terms of ease of administration and economy, the oral route is the preferred route of drug administration over other routes. Effective aqueous solubility is the first prerequisite for oral medication, since low solubility has poor absorption and bioavailability and unpredictable toxicity of the gastrointestinal mucosa. To avoid these crises, different methodologies are used to improve the solubility and bioavailability of poorly soluble drugs, and hydrotropic solubilization is one of them. Hydrotropic agents have the potential to improve the solubility of water-insoluble drugs. In this review, we try to address hydrotropic solubilization methodologies. Keywords: Hydrotropy, Micelles, Solubility, Formulation.


Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 101 ◽  
Author(s):  
Michael Brunsteiner ◽  
Johannes Khinast ◽  
Amrit Paudel

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.


2019 ◽  
Vol 13 (2) ◽  
pp. 91-104 ◽  
Author(s):  
Surya Goel ◽  
Monika Sachdeva ◽  
Vijay Agarwal

Background: Nanosuspension has arisen as a remunerative, lucrative as well as a potent approach to improve the solubility and bioavailability of poorly aqueous soluble drug entities. Several challenges are still present in this approach which need more research. The prime aim of this review is to identify such challenges that can be rectified in the future. Methods: Through this review, we enlighten the recent patents and advancement in nanosuspension technology that utilize the different drug moieties, instruments and characterization parameters. Results: Nanosuspension has been found to possess great potential to rectify the several issues related to poor bioavailability, site-specific drug delivery, dosing frequency, etc. In the past decade, nanosuspension approach has been complementarily utilized to solve the developed grievances, arisen from poorly soluble drugs. But this field still needs more attention to new discoveries. Conclusion: Nanosuspension contributes a crucial role in administering the different drug entities through a variety of routes involving oral, transdermal, ocular, parenteral, pulmonary, etc. with solving the different issues. This review also confirms the significance of nanosuspension in safety, efficacy, and communal as well as the economic expense associated with healthcare.


2012 ◽  
Vol 423 (2) ◽  
pp. 452-460 ◽  
Author(s):  
Nicolas Duhem ◽  
Julien Rolland ◽  
Raphaël Riva ◽  
Pierre Guillet ◽  
Jean-Marc Schumers ◽  
...  

2009 ◽  
Vol 7 (1) ◽  
pp. 227-236 ◽  
Author(s):  
Feng Wang ◽  
He Hui ◽  
Timothy J. Barnes ◽  
Christian Barnett ◽  
Clive A. Prestidge

2020 ◽  
Vol 13 (2) ◽  
pp. 80-93 ◽  
Author(s):  
Abikesh P.K. Mahapatra ◽  
Vinod Patil ◽  
Ravindra Patil

The primary aim of this review was to improve the solubility and Bioavailability of BCS Class-II drugs because of their low solubility and dissolution rate. Solubility is one of the imp parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. Hence the class- II drugs require enhancement in solubility and dissolution rate in there formulation development particularly in solid dosage form such as in tablet and capsule. So because of this there are several methods and newer emerging technologies have been developed for increasing the solubility as well as Bioavailability of class –II drugs. In this article review on literature on newer techniques or methods as well as recent research on formulation development of class- II drugs was done.


2017 ◽  
pp. 125-186
Author(s):  
Dev Prasad ◽  
Akash Jain ◽  
Sudhakar Garad

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