Abstract
Purpose: Neostigmine bromide, a cholinesterase inhibitor is conventionally given by oral route for the treatment of myasthenia gravis. However, it is very poorly absorbed from gastro-intestinal tract. Intranasal administration is an ideal alternative to the parenteral route for systemic drug delivery. Formulating multiparticulate system with mucoadhesive polymers may provide a significant increase in the nasal residence time. The aim of the present approach was to overcome the drawbacks of the conventional dosage forms of Neostigmine Bromide by formulating intranasal microspheres with Carbopol 974P NF and HPMC K15 M along with film forming polymer ethyl cellulose. Methods: The microspheres were prepared by emulsion solvent evaporation method. The prepared microspheres were characterized for encapsulation efficiency, drug loading, particle size, and surface morphology, degree of swelling, in-vitro mucoadhesion, drug release, in-vivo studies and stability studies. Results: Formulations IN 1 and IN 5 displayed the best results for Carbopol and HPMC based microspheres respectively. Entrapment efficiency was 75.74±0.50% and 70.27±0.61%; mucoadhesion was 98.5% and 85.3%; and drug release up to 8 h was 87.86% and 84.5% for IN 1 and IN 5 respectively. In-vivo studies revealed that the formulations IN 1 and IN 5 showed good bioavailability compared to oral drug administration. Conclusion: Both in-vitro and in-vivo studies conclude that Carbopol based microspheres are better than HPMC based microspheres for the delivery of Neostigmine Bromide.
Highlights
The most desirable and convenient method of drug administration is the oral route because of their ease of administration
The present study has been satisfactorily attempted to formulate a mucoadhesive microparticulate system of an anticholiesterase drug like Neostigmine Bromide for intranasal administration with a view of enhancing bioavailability of the drug. % entrapment efficiency was higher for Carbopol based microspheres than HPMC based microspheres
The particle size analysis revealed that all formulations gave particles in the range of 250-400 μm which is suitable for intranasal administration of formulation
Summary
The most desirable and convenient method of drug administration is the oral route because of their ease of administration. IN delivery is non-invasive, essentially painless, does not require sterile preparation, and is and readily administered by the patient or a physician, e.g., in an emergency setting. Given these positive attributes, it is logical to consider IN administration when developing new therapeutics, or when extending the life or improving the profile of an existing drug [4,5]. Subsequent to a drug’s passage through the mucus, there are several mechanisms for absorption through the mucosa These include transcellular or simple diffusion across the membrane (for lipophilic drugs), paracellular transport via movement between cell (for water soluble drugs) and transcytosis by vesicle carriers [6,7]
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