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1.
Drug Deliv Transl Res ; 10(4): 1136-1146, 2020 08.
Artigo em Inglês | MEDLINE | ID: mdl-32219727

RESUMO

The present study investigates the role of fish oil (FO)- and butter oil (BO)-enriched microemulsion-based system of galantamine hydrobromide (GH), an anti-Alzheimer drug, for its potential role in brain permeation enhancement and neuroprotection against oxidative stress. Microemulsion (ME)-based system of GH was prepared using water phase titration. The prepared ME was characterized by several physicochemical parameters like particle size, polydispersity index, and ex vivo drug permeation. Cell-based oxidative stress assays and pharmacokinetic studies were performed using C6 glial cell lines, and Sprague Dawley rats, respectively. The optimized ME comprised 5.3% v/v of Capmul MCM EP (as oil),15.8% v/v of Tween-80 (as surfactant), 5.3% v/v of Transcutol P (as co-surfactant), and 73.6% v/v of water (as aqueous phase). The addition of FO and BO resulted in a slight increase in the droplet size and decrease in transparency of ME. Cell-based anti-oxidative stress assays (glutathione assay, nitrite assay, and lipid peroxidation assay) showed the efficacy of formulation in the order of ME, BO ME, and FO ME, respectively. A similar trend was also observed in in vivo animal studies, wherein GH FO ME showed a comparatively higher percentage of drug reaching the brain when administered by intranasal route than by IV route. The study concluded the potential benefits of co-administering FO- and BO-enriched microemulsion is not only enhancing the permeation of drugs across BBB but also improving efficacy against lipopolysaccharide-induced oxidative stress. Graphical abstract.


Assuntos
Óleos de Peixe/administração & dosagem , Galantamina/administração & dosagem , Ghee , Fármacos Neuroprotetores/administração & dosagem , Administração Intranasal , Administração Intravenosa , Animais , Encéfalo/metabolismo , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Emulsões , Óleos de Peixe/química , Óleos de Peixe/farmacocinética , Galantamina/sangue , Galantamina/química , Galantamina/farmacocinética , Glutationa/metabolismo , Cabras , Lipopolissacarídeos , Malondialdeído/metabolismo , Fármacos Neuroprotetores/sangue , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/farmacocinética , Estresse Oxidativo/efeitos dos fármacos , Ratos Sprague-Dawley
2.
Nutrition ; 65: 138-157, 2019 09.
Artigo em Inglês | MEDLINE | ID: mdl-31132629

RESUMO

Since the discovery of fatty acids, a niche has been carved for their vital role as adjuvants in drug delivery and as treatment for various diseases. The literature has repeatedly described the essential role of various fatty acids in treating a wide range of diseases and disorders, from central nervous system diseases to wound healing. The use of fatty acids has expanded to many horizons and in recent decades they have gained importance as drug delivery adjuvants in addition to their auxiliary benefits in treating various diseases. Although fatty acids aid in solving both formulation-based and therapeutic challenges to our knowledge, they have never been viewed as dual agents in modern scientific literature. The aim of this review was to provide this perspective and combine the very discreet literature about fatty acids, which includes their role as therapeutic adjuvants and drug delivery agents. It gives insights on the use of fatty acids in treating the diseases of the eye, skin, central nervous system, viral diseases, and so on. The review further discusses how the structure of fatty acids plays an important role in therapeutic activity and affects formulation stability.


Assuntos
Adjuvantes Imunológicos/farmacologia , Sistemas de Liberação de Medicamentos , Ácidos Graxos/farmacologia , Humanos
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