Polysacchrides represent an important group of excipients. Particularly, cellulose and its derivatives are commonly used excipients for oral route of drug delivery. For oral delivery, cellulose derivatives are used to meet different requirements such as fillers, solubility and bioavailability enhancers of active pharmaceutical ingredients, ease manufacturing of dosage forms or to achieve certain release profile from formulations. Of particular interest is the use of cellulose derivatives to improve solubility and bioavilability of poorly water soluble drugs. It is estimated that approximately 40% of active substances currently in development fail because of low efficacy which can result from poor bioavailability arising from ineffective intestinal absorption and/or undesirable metabolic activity. To improve drug delivery, the amorphous form of a poorly water-soluble drug compound is often used to generate supersaturated solutions. The supersaturated solutions generated from the dissolution of amorphous solids may lead to an increase in absorption compared to that of a saturated solution if supersaturation can be maintained for a physiologically-relevant type period. However, to maintain supersaturation, crystallization (nucleation and crystal growth) must be prevented and polymeric additives, especially cellulose derivatives are used for this purpose. In addition, it has also been demonstrated that supersaturating bioactive delivery systems, consisting of amorphous solid dispersions of the poorly-water soluble compound with a water soluble polymer are capable of generating colloidal dispersions (nanosuspensions) when dissolved in aqueous solution and these dispersions are important to the bioavailability enhancement often seen with amorphous solid dispersions. In this presentation, an overview with case studies, of the different uses of cellulose derivatives in formulations for oral drug delivery in drug development will be discussed. The underlying factors that affect the ability of polymeric additives to inhibit nucleation and crystal growth for a given drug compound will be presented. In addition, we will also report on the use of cellulose derivatives to improve nanosuspension yield of amorphous solid disperions in aqueous solution thus improving bioavailability in preclinical studies.

Polyscaccharides in drug delivery: Applications of cellulose derivatives for oral drug delivery

253rd National Meeting (2017)

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