Development and optimization of RofA-PAMAM dendrimer complex materials for sustained drug delivery

Abstract

The current indagation is observed on anatomization of drug release dynamics aiming at preceding the anti-inflammation activity of roflumilast analogue (RofA), post assemblage with dendrimer. The study pondered the development and optimization of RofA-Dendrimer complexes for sustained delivery. Many physiological and physicochemical factors, like encapsulation potency, drug loading, drug release, dissolvability, stability, and anti-inflammation activity were determined. The study results in the observation of encapsulation potency of 72.64 ± 0.189%, loading capability of 63.41 ± 0.166%, and in vitro release of RofA-4.0 G PAMAM complex was found to increase making it an appropriate candidate for sustained drug release progressively . It has been found by constructing drug release kinetics, that the release followed was a non- fickian diffusion ( n<0.89). The phase solubility diagram indicated an increment of solubility of RofA with varied dendrimer generation as well as pH. The study was initiated to prepare a suited candidate fit to scale back site-specific inflammation. Further concluding the contemplation for its sustained delivery, enhanced solubility, and potentially augmented anti-inflammation activity. • The aims of this study were to assess the potentially augmented effect of roflumilast analogue post assemblage with different generations of polyamidoamine dendrimer. • In this study, RofA-Dendrimer complexes, with RofA as the model drug, the encapsulation potency, loading capacity, in vitro drug release behavior, and stability were studied. • The effect of the concentration of varied generations of PAMAM dendrimer on the solubility of RofA has been discussed in detail. • We also examined the anti-inflammatory activity and sought to determine the inhibitory effect on protein denaturation. • The results were affirmed by the determination of n value i.e. hill coefficient with respect to the substrate concentration and rate of inhibition. • The impact of adjuvant antibiotic therapy was also explored by the means of a cytotoxicity assay.