Preparation and Evaluation of PLGA-Coated Capsaicin Magnetic Nanoparticles.
Drugs used in the treatment of diseases can cause several unwanted systemic side effects. A site-specific drug delivery system can eliminate such consequences by delivering drugs to certain target areas of the body where therapeutic effects are required. Here we present the preparation and evaluation of magnetic nanoparticles of capsaicin, the active ingredient in chili peppers, coated with poly-L-lactide co-glycolide (PLGA), a FDA-approved biodegradable bioavailable polymer.



PCMN were prepared by solvent-evaporation/coprecipitation technique and their physicochemical and pharmacological characteristics evaluated in vitro. Further, effective pain/inflammation therapeutics of PCMN in a mouse model of inflammation was also studied. We also prepared and evaluated the subcellular localization of PLGA coated fluorescence magnetic nanoparticle (PFMN) in vitro in HEK293 cells.



Transmission electron microscopic images of PCMN showed that the size of the nanoparticles were of the order of 10-20 nm. PCMN showed approximately 9.29% drug loading and 89.15% encapsulation efficiencies. In vitro dissolution studies showed an increased solubility of capsaicin due to the nano-size of the PCMN, while PLGA coating allowed sustained release of capsaicin in vitro. The PCMN also reduced paw edema after injection in mice, and confocal microscopy revealed the successful intracellular localization of PLGA-coated fluorescein magnetic nanoparticles in HEK293 cells.



The PCMN provided a sustained release of capsaicin in vitro and inhibited carrageenan-induced inflammatory pain in mouse model in vivo. These data suggest that PLGA coating of capsaicin magnetic nanoparticles have the potential to be amenable for a sustained release of capsaicin to relieve pain.
School of Pharmacy, University of Wyoming, 1000 East University Avenue, Laramie, Wyoming, 82071, USA.|Princeton University, Princeton, New Jersey, USA.
Mrudhula
M
Baskaran
School of Pharmacy, University of Wyoming, 1000 East University Avenue, Laramie, Wyoming, 82071, USA.
Padmamalini
P
Baskaran
Department of Chemistry, University of Wyoming, 1000 East University Avenue, Laramie, Wyoming, 82071, USA.
Navamoney
N
Arulsamy
School of Pharmacy, University of Wyoming, 1000 East University Avenue, Laramie, Wyoming, 82071, USA. Baskaran.Thyagarajan@uwyo.edu.|Molecular Signaling Laboratory, School of Pharmacy, University of Wyoming, 1000 East University Avenue, Laramie, Wyoming, 82071, USA. Baskaran.Thyagarajan@uwyo.edu.
Baskaran
0000-0002-4757-6125
B
Thyagarajan
D000818:Animals; D002211:Capsaicin / Q000737:chemistry / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D065546:Drug Liberation; D019793:Fluorescein / Q000737:chemistry; D005456:Fluorescent Dyes / Q000737:chemistry; D057809:HEK293 Cells; D006801:Humans; D007249:Inflammation / Q000188:drug therapy; D019344:Lactic Acid / Q000737:chemistry*; D058185:Magnetite Nanoparticles / Q000737:chemistry*; D008297:Male; D008810:Mice, Inbred C57BL; D010146:Pain / Q000188:drug therapy*; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D012995:Solubility; D013499:Surface Properties
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005456:Fluorescent Dyes; D058185:Magnetite Nanoparticles; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D002211:Capsaicin; D019793:Fluorescein
PLGA; TRPV1; capsaicin; magnetic nanoparticles; pain