scholarly journals Bioavailability Improvement Strategies for Poorly Water-Soluble Drugs Based on the Supersaturation Mechanism: An Update

2016 ◽  
Vol 19 (2) ◽  
pp. 208 ◽  
Author(s):  
Meiyan Yang ◽  
Wei Gong ◽  
Yuli Wang ◽  
Li Shan ◽  
Ying Li ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Water Soluble ◽  
Formulation Development ◽  
Equilibrium Solubility ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Soluble ◽  
Poorly Water Soluble

The formulation development for poorly soluble drugs still remains a challenge. Supersaturating drug delivery systems (SDDS) or drug delivery systems based on supersaturating provide a promising way to improve the oral bioavailability of poorly water-soluble drugs. In supersaturable formulations, drug concentration exceeds the equilibrium solubility when exposed to gastrointestinal fluids, and the supersaturation state is maintained long enough to be absorbed, resulting in compromised bioavailability. In this article, the mechanism of generating and maintaining supersaturation and the evaluation methods of supersaturation assays are discussed. Recent advances in different drug delivery systems based on supersaturating are the focus and are discussed in detail.This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

scholarly journals Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs

2013 ◽  
Vol 63 (4) ◽  
pp. 427-445 ◽  
Author(s):  
Katja Čerpnjak ◽  
Alenka Zvonar ◽  
Mirjana Gašperlin ◽  
Franc Vrečer
Keyword(s):  
Drug Delivery ◽  
Oral Bioavailability ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Pharmaceutical Products ◽  
Delivery Systems ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Abstract Low oral bioavailability as a consequence of low water solubility of drugs is a growing challenge to the development of new pharmaceutical products. One of the most popular approaches of oral bioavailability and solubility enhancement is the utilization of lipid-based drug delivery systems. Their use in product development is growing due to the versatility of pharmaceutical lipid excipients and drug formulations, and their compatibility with liquid, semi-solid, and solid dosage forms. Lipid formulations, such as self-emulsifying (SEDDS), self-microemulsifying SMEDDS) and self- -nanoemulsifying drug delivery systems (SNEDDS) were explored in many studies as an efficient approach for improving the bioavailability and dissolution rate of poorly water-soluble drugs. One of the greatest advantages of incorporating poorly soluble drugs into such formulations is their spontaneous emulsification and formation of an emulsion, microemulsion or nanoemulsion in aqueous media. This review article focuses on the following topics. First, it presents a classification overview of lipid-based drug delivery systems and mechanisms involved in improving the solubility and bioavailability of poorly water-soluble drugs. Second, the article reviews components of lipid-based drug delivery systems for oral use with their characteristics. Third, it brings a detailed description of SEDDS, SMEDDS and SNEDDS, which are very often misused in literature, with special emphasis on the comparison between microemulsions and nanoemulsions.

scholarly journals Hydrogel-Based Drug Delivery Systems for Poorly Water-Soluble Drugs

Molecules ◽  
2015 ◽  
Vol 20 (11) ◽  
pp. 20397-20408 ◽  
Author(s):  
Matthew McKenzie ◽  
David Betts ◽  
Amy Suh ◽  
Kathryn Bui ◽  
London Kim ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

scholarly journals Lipid-Based Drug Delivery Systems

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Hina Shrestha ◽  
Rajni Bala ◽  
Sandeep Arora
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Parenteral Delivery ◽  
Wide Range ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Principle Objective

The principle objective of formulation of lipid-based drugs is to enhance their bioavailability. The use of lipids in drug delivery is no more a new trend now but is still the promising concept. Lipid-based drug delivery systems (LBDDS) are one of the emerging technologies designed to address challenges like the solubility and bioavailability of poorly water-soluble drugs. Lipid-based formulations can be tailored to meet a wide range of product requirements dictated by disease indication, route of administration, cost consideration, product stability, toxicity, and efficacy. These formulations are also a commercially viable strategy to formulate pharmaceuticals, for topical, oral, pulmonary, or parenteral delivery. In addition, lipid-based formulations have been shown to reduce the toxicity of various drugs by changing the biodistribution of the drug away from sensitive organs. However, the number of applications for lipid-based formulations has expanded as the nature and type of active drugs under investigation have become more varied. This paper mainly focuses on novel lipid-based formulations, namely, emulsions, vesicular systems, and lipid particulate systems and their subcategories as well as on their prominent applications in pharmaceutical drug delivery.

scholarly journals Cyclodextrin based nanosponges for pharmaceutical use: A review

2013 ◽  
Vol 63 (3) ◽  
pp. 335-358 ◽  
Author(s):  
Gursalkar Tejashri ◽  
Bajaj Amrita ◽  
Jain Darshana
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Drug Loading ◽  
Delivery Systems ◽  
Water Soluble ◽  
Pharmacokinetic Parameters ◽  
Prolonged Release ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Abstract Nanosponges are a novel class of hyper-crosslinked polymer based colloidal structures consisting of solid nanoparticles with colloidal sizes and nanosized cavities. These nano-sized colloidal carriers have been recently developed and proposed for drug delivery, since their use can solubilize poorly water-soluble drugs and provide prolonged release as well as improve a drug’s bioavailability by modifying the pharmacokinetic parameters of actives. Development of nanosponges as drug delivery systems, with special reference to cyclodextrin based nanosponges, is presented in this article. In the current review, attempts have been made to illustrate the features of cyclodextrin based nanosponges and their applications in pharmaceutical formulations. Special emphasis has been placed on discussing the methods of preparation, characterization techniques and applications of these novel drug delivery carriers for therapeutic purposes. Nanosponges can be referred to as solid porous particles having a capacity to load drugs and other actives into their nanocavity; they can be formulated as oral, parenteral, topical or inhalation dosage forms. Nanosponges offer high drug loading compared to other nanocarriers and are thus suitable for solving issues related to stability, solubility and delayed release of actives. Controlled release of the loaded actives and solubility enhancement of poorly water-soluble drugs are major advantages of nanosponge drug delivery systems.

scholarly journals Nanosuspensions as a promising approach to enhance bioavailability of poorly soluble drugs : An update

2019 ◽  
Vol 9 (2) ◽  
pp. 574-582
Author(s):  
Stanekzai Azimullah ◽  
, Vikrant ◽  
CK Sudhakar ◽  
Pankaj Kumar ◽  
Akshay Patil ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Water Soluble ◽  
Wet Milling ◽  
Poorly Water Soluble Drugs ◽  
Limited Applicability ◽  
Water Soluble Drugs ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
Emulsification Solvent Evaporation ◽  
Biphasic Systems

Solubility is a vital factor for devloping drug delivery systems for poorly water soluble drugs. Several conventional approaches for enhancement of solubility have limited applicability, especially when the drugs are poorly water soluble. Nanosuspension technology can be used to enhance the solubilty, stability as well as the bioavailability of poorly water soluble drugs. Nanosuspensions are biphasic systems comperising of pure drug particles dispersed in an aqueous vehicle, stabilized by surfac active agents. Fabrication of nanosuspension is simple and more advantageous than other approaches. Techniques like high-pressure homogenization, wet milling, emulsification, solvent evaporation, bottom up technology and top down technology have been applicable in the fabrication of nanosuspensions. Nanosuspension delivery is possible by several routes, such as oral, pulmonary, parenteral and ocular routes. Nanosuspension not only solves solubility and bioavailability issue, but improve drug safety and efficacy. In this context, we reviewed the current techniques used to develop nanosuspensions and their recents studies application in drug delivery system. Keywords : Solubility, fabrication, Characterization, Applications, Nanosuspension.

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