Background: Camptothecin is known for its potent anticancer activity. However, its optimal activity
is reduced due to its low solubility and stability in biological media.
Objective: The aim of the present study is to design and characterize a Camptothecin (CPT) suppository formulation.
Methods: Rectal suppositories of camptothecin alone, encapsulated with Cyclodextrin (CD) and in the ternary
system (CPT encapsulated with cyclodextrin and dispersed in Polyethylene Glycol (PEG) 6000) were prepared
using various hydrophobic and hydrophilic polymeric bases as semi-synthetic glyceride (Suppocire® AM Pellets)
and Polyethylene Glycols (PEGs) mixtures. Formulations were evaluated by various parameters like weight
variation, drug content, hardness and liquefaction time. In vitro release study was performed in USP type I apparatus
using phosphate buffer pH 7.2 as dissolution media.
Results: Suppositories were within the permissible range of all physical parameters. In vitro drug released from
water soluble base (PEG) was greater than that from oil soluble base with ninety percent (90%) of drug dissolution.
It was also established that drug release from various formulations was by diffusion mechanism, according
to the Higuchi’s equation.
Conclusion: This new formulation offers a new approach to colorectal cancer treatment by offering an alternative
and simple drug administration route.