Study of mucoadhesive microsphere of pirfenidone for nasal drug delivery

Abstract

T he present research work involves formulation development and evaluation of nasal mucoadhesive microsphere in view to, improve bioavailability and reduce dosing regimen. Microspheres were prepared by spray drying and cross-linking method using chitosan and HPMC K4M, using 32 central composite design. Microspheres were evaluated for particle size, drug content, swelling ability, and percentage yield. Compatibility was checked by doing Fourier transform infrared spectroscopy and Differential scanning calorimetry study. The polymorphism and particle shape were studied by X-ray diffraction and scanning electron microscopy. The average particle size of spray-dried and cross-linked formulations were found in the range between 20-50 µm and 30-60 µm with percent mucoadhesion in the range of 80%-90% and 60-70%, respectively. In vitro drug release was found to be proportional to drug to polymer ratio. In vitro drug release for optimized formulation, that is, (F1), for spray-drying method and cross-linking method was found to be 88.73% and 70.93% at the end of 6 h, respectively. Release of drug from microspheres followed non-Fickian diffusion kinetics. Ex vivo studies were performed with sheep nasal mucosa for mucoadhesion, histopathological study, and drug permeation. The histopathological study indicates nonirritant nature of microsphere. The microspheres were found to be stable at accelerated storage conditions for 1 month, as per International Conference of Harmonisation guidelines.

Dual drug-loaded coaxial nanofibers for the treatment of corneal abrasion

“…However, for the pure pirfenidone and moxifloxacin, a very clear characteristic reflection is observed in their XRD pattern. Distinct peaks at 8.90º, 14.94º, 19.04º, 23.08º, 24.80º and 27.60º were observed in pirfenidone diffractogram, which is similar to the findings of Kashikar et al (2014) and Soni et al (2018) pirfenidone diffractograms. The moxifloxacin XRD pattern showed diffraction peaks at 5.90º, 8.62º, 11.81º, 14.48º, 15.58º, 17.34º, 24.18º, 26.60º, 27.46º and 31.54º, which are in agreement with the moxifloxacin XRD pattern of Mudgil and Pawar (2013).…”

Development of a Long-Term Drug Delivery System with Levonorgestrel-Loaded Chitosan Microspheres Embedded in Poly(vinyl alcohol) Hydrogel

“…Biodegradable microsphere drug reservoirs, formulated using natural or synthetic polymers, have been used for sustained release of different contraceptive drugs. ,,, Emulsion-based cross-linking methods have been widely used to prepare microspheres for controlled drug delivery systems, including (i) short-term release microspheres such as pullulan-poly­(vinyl alcohol) (PVA) microsphere emulsion cross-linked by glutaraldehyde (GA) to release pirfenidone in lungs in 24 h, chitosan (CS) microspheres cross-linked by GA for pirfenidone nasal delivery in 6 h, and acrylamide-grafted locust bean gum (Am- g -LBG) and poly­(vinyl alcohol) (PVA) microspheres for buflomedil hydrochloride oral delivery in 12 h; (ii) sustained release microspheres such as poly­(ε-caprolactone) (PCL) microspheres with levonorgestrel (LNG) for long-term release of 120 days, , poly­(lactic- co -glycolic acid) (PLGA) microspheres coated with PVA hydrogel for the sustained dexamethasone release in one month . The drug release behavior from microsphere systems, such as the release rate, duration of action, initial burst release, and overall in vitro/in vivo correlation, can be altered by the microsphere composition, cross-linking method/density, particle size, shape, molecular weight, the drug loading and distribution, and the fabrication and sterilization processes. ,− With the above-mentioned text taken into account, in this study, CS, a natural biodegradable polysaccharide obtained by alkaline deacetylation of chitin, was cross-linked by GA and synthesized as a microsphere reservoir for the contraceptive drug LNG.…”

HPMC K15M and Carbopol 940 mediated fabrication of ondansetron hydrochloride intranasal mucoadhesive microspheres

“…and techniques (spray-drying method, etc. ); a sharp contrast in results were observed (Nanjwade et al, 2011;Jain et al, 2009;Kashikar et al, 2014;Shashi et al, 2011;Jain et al, 2012). The solvent evaporation technique employed for fabricating the OH mucoadhesive microspheres utilizing HPMC and Cb described an imperative method with high yield, better mucoadhesivity, higher drug loading with enhanced percentage entrapment, etc than the previous reports (Dandge and Dehghan, 2009;Mahajan et al, 2008).…”