Design and optimization of cyclodextrin-based nanosponges of antimalarials using central composite design for dry suspension

Abstract

The hyper cross-linked nanoporous architecture of nanosponges plays a vital role in the development of dosage forms. The innate nature of nanosponges facilitates controlled release profile, chemical stability and taste masking. The current study aimed to synthesize cyclodextrin-based artemether-lumefantrine nanosponges using central composite design as an optimization tool and show their application in the formulation of dry suspension. The cyclodextrins-based nanosponges of artemether-lumefantrine were synthesized using the solvent evaporation method. The optimized nanosponges were characterized by TEM, DSC, XRPD, FTIR, etc. The statistically optimized nanosponge formulation showed a particle size of 335 ± 2.4 nm and percentage entrapment efficiency (% EE) of 69.2 ± 1.6% and 89.6 ± 3.1% for the artemether and lumefantrine, respectively. The formulated suspension was evaluated for taste, sedimentation volume, redispersibility, in-vitro release and chemical stability and exhibited results within acceptable limits. Dry suspension showed a controlled release profile with 89.8 ± 3.2% and 97.7 ± 4.1% release at 24 h for artemether and lumefantrine, respectively. Dry suspension of artemether-lumefantrine-loaded nanosponges presents a contemporary approach and extends their potential in the development of controlled-release suspension of Biopharmaceutical Classification System (BCS) class II and IV drugs.