Abstract
Adequate aqueous solubility has been one of the desired properties while selecting drug molecules and other bio-actives for product development. Often solubility of a drug determines its pharmaceutical and therapeutic performance. Majority of newly synthesized drug molecules fail or are rejected during the early phases of drug discovery and development due to their limited solubility. Sufficient permeability, aqueous solubility and physicochemical stability of the drug are important for achieving adequate bioavailability and therapeutic outcome. A number of different approaches including co-solvency, micellar solubilization, micronization, pH adjustment, chemical modification, and solid dispersion have been explored toward improving the solubility of various poorly aqueous-soluble drugs. Dendrimers, a new class of polymers, possess great potential for drug solubility improvement, by virtue of their unique properties. These hyper-branched, mono-dispersed molecules have the distinct ability to bind the drug molecules on periphery as well as to encapsulate these molecules within the dendritic structure. There are numerous reported studies which have successfully used dendrimers to enhance the solubilization of poorly soluble drugs. These promising outcomes have encouraged the researchers to design, synthesize, and evaluate various dendritic polymers for their use in drug delivery and product development. This review will discuss the aspects and role of dendrimers in the solubility enhancement of poorly soluble drugs. The review will also highlight the important and relevant properties of dendrimers which contribute toward drug solubilization. Finally, hydrophobic drugs which have been explored for dendrimer assisted solubilization, and the current marketing status of dendrimers will be discussed.
Highlights
The role of aqueous-solubility of any new chemical entity (NCE) or a drug is crucial and decisive in the development of its formulation
A report published by Benet et al (2011), which categorized 698 commercially available, orally administered immediaterelease (IR) drugs using the Biopharmaceutics Drug Disposition Classification System (BDDCS), stated 33% of those drugs to be under BCS (Biopharmaceutical classification system) ClassII, and 6% of those drugs to be under BCS Class IV (Benet et al, 2011)
The report estimated that only 5% of new molecular entities (NMEs) under development by industry had both high solubility and high permeability (BCS Class I), while another 5% were of BCS Class III
Summary
The role of aqueous-solubility of any new chemical entity (NCE) or a drug is crucial and decisive in the development of its formulation. The report estimated that only 5% of new molecular entities (NMEs) under development by industry had both high solubility and high permeability (BCS Class I), while another 5% were of BCS Class III. 70% of NMEs under investigation/development were BCS Class II compounds and 20% were BCS Class IV compounds (Benet et al, 2011). Though many of these entities are highly potent drug candidates, they are not taken further into the development due to their limited aqueous solubility. In the recent years several efforts have been made to solubilize hydrophobic drugs; some of those strategies are briefly discussed
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