Abstract

Objective: In the domain of nano drug delivery, dendrimers are the most explored bioactive polymeric carrier system. The present work was aimed to study the diffusion potential of different generations of Poly (propyleneimine) (PPI) dendrimers on goat nasal mucosa in an ex vivo study and synthesize a stable dendrimer for olfactory drug delivery.Methods: The generations (3.0G, 4.0G, and 5.0G) of PPI dendrimer were synthesized, and PEGylated by MPEG 5000 and then loaded with donepezil. A comparative study was carried out among all generations in term of their drug loading capacity, stability, sustained release behaviour as well as for targeting efficacy. An ex-vivo study was carried out on Franz Diffusion Cell with goat nasal mucosa.Results: The developed G3, G4, and G5 dendrimerformulations had entrapment efficiency of 24.33±0.56%, 40.12±0.62%, and 60.4±0.6%, respectively. The nasal diffusion study revealed that 5.0G PPI dendrimer increased diffusion of donepezil up to 47% as compared to the pure solution of donepezil while 10% improvement in diffusion was seen as compared to 4.0 G PPI dendrimer. Thus obtained results claimed that the drug loading as well as targeting potential of PPI dendrimers increased with the increase in the number of generation. The investigation outcome indicated promising results of 5.0G PPI dendrimer over the 3.0G and 4.0G PPI dendrimer generations for their drug loading capacity, stability, and sustained release action.Conclusion: The 5.0G PPI dendrimer proved its superior candidature over the other lower generations of PPI dendrimers for drug delivery and drug targeting.

Highlights

  • A drug delivery system administers therapeutic agents in the body

  • The present study investigates the targeting potential as well as biocompatibility of different generations of PPI dendrimers

  • FT-IR and 1H-NMR spectroscopic methods wereused to confirm the synthesis of every generation and elucidate the structure of synthesized dendrimeric generation

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Summary

Introduction

A drug delivery system administers therapeutic agents in the body. The delivery system changes pharmacokinetic as well as pharmacodynamic behaviour of therapeutics and enhances its pharmacological activities provide maximum benefits. Nature and sources the drug delivery system may have various devices for administration. The traditional drug delivery system has various agents like micro-emulsion, tablets, capsules, ointments, microparticles and multiple emulsions depending on their size [1,2,3]. Nanotechnology offers exquisite approaches such as nanoparticles, dendrimers, liposomes and carbon nanotubes etc [4, 5]. The nanocarriers may be validated and designed with defined size, shape and surface charge etc. Claim their potential in targeted as well as controlled drug delivery The nanocarriers may be validated and designed with defined size, shape and surface charge etc. and claim their potential in targeted as well as controlled drug delivery

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