1. Gaurav Mittal and Aseem Bhatnagar
DEVELOPMENT OF NANO-SALBUTAMOL SULPHATE DPI FOR THE TREATMENT OF ASTHMA & LUNG INJURIES
Braj Gaurav Sharma*, Bhavna, Neeraj Kumar, Thakuri Singh, Dhruv K Nishad, Amit Tyagi,
Gaurav Mittal and Aseem Bhatnagar
Institute of Nuclear Medicine and Allied Sciences (DRDO) Brig. SK Mazumdar Marg, Delhi-54, India
Author :
Defence R&D Organisation
Institute of Nuclear Medicine & Allied Sciences
INTRODUCTION
4. In-vitro aerodynamic particle size distribution using Anderson Cascade Impactor (ACI)
3.In-vitro aerodynamic particle size distribution using Anderson Cascade Impactor
Respiratory diseases i.e. Ashthma/COPD are more common at high altitude. Salbutamol (INN)) is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease.
We have optimized the protocols for synthesis of salbutamol sulphate nanoparticles using Nano-Technolgy. The results obtained will be of immensely helpful for clinicians to predict response of patients to salbutamol sulphate nano-DPI. Developed formulation will be useful for high altitude application.
Aerodynamic particle size distribution and dose proportionality of Nano salbutamol was quantified using ACI using radiometry as well as spectroscopy techniques. The flow rate was maintained at 28.3 L/min
5.Gamma scintigraphy study of 99mTc-labeled Nano-salbutamol in healthy human volunteers
Human volunteers were inhaled radiolabeled Nano-salbutamol by Rotahaler® to quantify pulmonary deposition of the drug. Each volunteer inhaled 1 puffs in single dose. Scintigraphy was used to estimate inhaled drug in lungs, trachea, oesophagus, mouth and GIT.
OBJECTIVE
Optimization of methodology for developing Nano particle of salbutamol sulphate.
Radiolabeling optimization and Serum stability studies of radiolabeled drug
Lung deposition studies of drug in healthy volunteers using scintigraphy
4.Gamma scintigraphy study of radiolabeled Nano-salbutamol sulphate in healthy human volunteers.
EXPERIMENTAL
RESULTS AND DISCUSSION
0 min
60 min
240 min
240 min
Micronised
Salbutamol
Nano-SBM
Particle
2. Radiolabelling of Nano-salbutamol: The drug was successfully radiolabeled with 99mTc-DTPA using stannous salt as reducing agent
3. Labeling efficiency: Labeling efficiency was ascertained by ITLC-SG chromatography using 100 % acetone as mobile phase
1. Prepreation of Nano partical of drug: Drug was dispersed in a solvent by anti-solvent precipitation technique to form a Nano suspension and dry Nano-particles were generated by spray drying.
1. Radiolabeling efficiency of Nano-salbutamol
Hydrosol Nano Suspention
Drug Solution
Micro-Mixing
Antisolvent
0 min
60 min
240 min
Nano-Salbutamol
Solvent evaporation by spray drying
Radiolabeling efficiency was consistently > 97% as ascertained by ITLC using 100 % acetone as mobile phase
99mTc-DTPA
Reducing agent
Nano-SBM
99mTc-Nano SBM
Reducing agent
CONCLUSION
2. Serum stability studies at 370C
Salbutamol sulphate nano particles were developed by solvent-antisolvent method and characterized using pharmacoscintigraphy.
Nano particles of salbutamol were radiolabeled with 99mTc-DTPA with good labeling efficiency & stability
Respiratory fraction & MMAD of the Nano drug using Rotahaler was found to be 45.2% & 1.61 µm respectively, as estimated by ACI studies while it was found 31.1% and 3.08 µm for micronized drug formulation.
Scintigraphy studies in human volunteers have shown 3 fold increased deposition of the nano drug in lungs, depicting its usefulness in treatment of asthma & pulmonary diseases.
99mTc-Nano SBM was found to be fairly stable in vitro as well as in vivo and the stability in serum indicated that 99mTc labeled drug remained bound to the chelate up to 24 hrs
Acknowledgement: Authors are thankful to Director, INMAS (DRDO)
National Workshop on Nanotechnology-2011 (For Defence Applications)
SSPL (DRDO)16-17 November 2011
REFERENCES