title: Cromolyn sodium encapsulated PLGA nanoparticles: An attempt to improve intestinal permeation.
abstract: High hydrophilicity curtails the intestinal permeation of cromolyn sodium (CS) which in turn compels to compromise with its multiple biological activities. Hence, the present research was intended with an objective to develop CS encapsulated polylactide-co-glycolide (PLGA) nanoparticles (CS-PNs) for enhancing intestinal permeation. The CS-PNs were prepared by double emulsification solvent evaporation method (W1/O/W2). The "Quality by Design" approach using box-behnken experimental design was employed to enhance encapsulation of CS inside CS-PNs without compromising with particle size. The polymer concentration, surfactant concentration and organic/aqueous phase ratio significantly affected the physicochemical properties of CS-PNs. The optimized CS-PNs were subjected to various solid-state and surface characterization studies using FTIR, DSC, XRD, TEM and AFM, which pointed towards the encapsulation of CS inside the spherical shaped nanoparticles without any physical as well as chemical interactions. Ex-vivo intestinal permeation study demonstrated ∼4 fold improvements in CS permeation by forming CS-PNs as compared to pure CS. Further, in-vivo intestinal uptake study performed using confocal microscopy, after oral administration confirmed the permeation potential of CS-PNs. Thus, the findings of the studies suggest that CS-PNs could provide a superior therapeutic carrier system of CS, with enhanced intestinal permeation.
authors.affiliation: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi 221 005 (U.P), India.
authors.forename: Ravi R
authors.initials: RR
authors.lastname: Patel
authors.affiliation: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi 221 005 (U.P), India.
authors.forename: Sundeep
authors.initials: S
authors.lastname: Chaurasia
authors.affiliation: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi 221 005 (U.P), India.
authors.forename: Gayasuddin
authors.initials: G
authors.lastname: Khan
authors.affiliation: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi 221 005 (U.P), India.
authors.forename: Pramila
authors.initials: P
authors.lastname: Chaubey
authors.affiliation: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi 221 005 (U.P), India.
authors.forename: Nagendra
authors.initials: N
authors.lastname: Kumar
authors.affiliation: Department of Pharmaceutics, Indian Institute of Technology (Banaras Hindu University), Varanasi 221 005 (U.P), India. Electronic address: bmishrabhu@rediffmail.com.
authors.forename: Brahmeshwar
authors.initials: B
authors.lastname: Mishra
mesh_terms: D000818:Animals; D001692:Biological Transport; D002214:Capsules; D004205:Cromolyn Sodium / Q000737:chemistry* / Q000378:metabolism*; D004337:Drug Carriers / Q000737:chemistry*; D005260:Female; D007413:Intestinal Mucosa / Q000378:metabolism*; D019344:Lactic Acid / Q000737:chemistry*; D008297:Male; D010316:Particle Size; D010539:Permeability; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats
chemical_list: D002214:Capsules; D004337:Drug Carriers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D004205:Cromolyn Sodium
keywords: Cromolyn sodium; Intestinal permeation; PLGA nanoparticles