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The aim of this study was to investigate whether floating microspheres prepared from polymer blends of hydroxypropyl methylcellulose in combination with either Eudragit S100 or Eudragit RS100 could improve the systemic bioavailability of the antiemetic drug; meclizine HCl (MCZ). Floating microspheres containing MCZ were prepared by emulsion solvent evaporation method. The influence of different polymer blend compositions on various formulation parameters and in vitrorelease characteristics of the prepared microspheres was investigated. In addition, the in vivopharmacokinetic profile of an optimized formula was evaluated. The mean particle size of prepared microspheres ranged from 290 to 383 μm. The percent drug entrapment efficiency varied between 51.9 ± 0.3% to 91.6 ± 0.7%. The formulated microspheres exhibited excellent floating ability. In vitrorelease profiles of floating microspheres indicated a rapid initial release followed by a sustained drug release for up to 24 h. The pharmacokinetic data affirmed the sustained effect of the optimized formula as indicated by the prolonged tmax, compared to the plain drug. Furthermore, the optimized formula showed higher relative bioavailability (154.25%), compared to the plain drug. These results suggest that MCZ floating microspheres might represent potential alternative to conventional MCZ oral formulations, with a higher and sustained therapeutic efficacy.

Fast disintegrating tablets (FDTs) dissolve or disintegrate in the mouth without the need of additional water. The aim of the present study was to formulate FDTs of Valsartan for the treatment of hypertension in children who could find difficulties in swallowing conventional solid dosage forms. The tablets were prepared by wet granulation technique. Superdisintegrants such as sodium starch glycolate (SSG) and crospovidone were optimized as 5% on the basis of least disintegration time. Different binders such as gelatin and HPMC k15m, at varying concentrations, were used along with the optimized superdisintegrant concentration. All the formulations were evaluated for content uniformity, disintegration time, friability, hardness and in vitrodissolution. In addition, the antihypertensive efficacy of optimized formulation(s) was investigated in vivo. The results of the physical parameters were found to be within the acceptable range. In vitrodissolution studies showed that increasing the concentration of superdisintegrant decreased the disintegration time, and thereby, promoted faster drug release from tablets. On the other hand, increasing binder concentration adversely hindered drug release from the tested formulations. Of interest, optimized formulation(s) of Valsartan FDTs rapidly and efficiently reduced the blood pressure in hypertensive rats. Collectively, FDTs could represent a potential drug delivery vehicle for the management of pediatric hypertension, in tandem with, alleviating the problems encountered with the administration of conventional oral solid dosage forms to children.

Breast cancer is the second most common cancers among female worldwide. The current treatment strategies includes surgery, chemo-, radio- and hormone-therapy. Nevertheless, breast cancer still accounts for more than 20% of all female cancer deaths, presumably, due to the lack of specificity to target site or the development of drug resistance. Graphene nanoribbons (GNRs) are one of the promising platforms that show efficient cellular internalization and high target specificity for cancer cells. Herein, oxidized graphene nanoribbons (OGNRs), decorated with folic acid (FA) and loaded with the selective estrogen receptor modulator, tamoxifen citrate (TC), were prepared from multi-walled carbon nanotubes using the longitudinal unzipping method. The synthesized TC-loaded OGNRs-FA showed multi-layered structure with drug loading efficiency of 56%. In vitrorelease studies showed a pH-dependent release of TC from OGNRs. In addition, TC loaded onto OGNRs significantly reduces cell viability and induces apoptosis in MCF-7 and MDA-MB-231 breast cancer cell lines in concentration and-time dependent manner. Most importantly, cellular uptake studies revealed that surface decoration of OGNRs with FA significantly contributed to the preferential cellular internalization of TC-loaded OGRNs-FA by breast cancer cells, compared to naked OGNRs. In vivopharmacokinetic study suggests that drug loading onto OGNRs-FA remarkably reduced the premature drug release in systemic circulation and, consequently, could enhance the availability of drug payload at the target site. Collectively, OGNRs-FA might represent a promising platform for efficient and selective delivery of tamoxifen to breast cancer cells. However, deep understanding of the in vivofate and long-term toxicity of OGNRs-FA is crucial for further clinical application.