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Pain Allaying Epalrestat-Loaded Lipid Nanoformulation for the Diabetic Neuropathic Pain Interventions: Design, Development, and Animal Study.
Vishwakarma, Vishal Kumar; Paswan, Shravan Kumar; Arora, Taruna; Verma, Rahul Kumar; Yadav, Harlokesh Narayan.
Afiliación
  • Vishwakarma VK; Department of Pharmacology, All India Institute of Medical Sciences (AIIMS), New Delhi 110029, India.
  • Paswan SK; Department of Pharmacology, All India Institute of Medical Sciences (AIIMS), New Delhi 110029, India.
  • Arora T; RBMCH, ICMR-Head Quarter's Ansari Nagar, New Delhi-110029, India.
  • Verma RK; Institute of Nano Science and Technology (INST), Phase-10, Sector-64, Mohali, Punjab 160062, India.
  • Yadav HN; Department of Pharmacology, All India Institute of Medical Sciences (AIIMS), New Delhi 110029, India.
Curr Drug Metab ; 23(7): 571-583, 2022.
Article en En | MEDLINE | ID: mdl-35950248
ABSTRACT

BACKGROUND:

Diabetic peripheral neuropathy is the most common complication of diabetes mellitus. Epalrestat, an aldose reductase inhibitor, has been approved for clinical therapy for diabetic peripheral neuropathic pain. In the present study, solid lipid-based nanoparticles are used for oral administration of epalrestat (E-SLN) and evaluated against diabetic neuropathic pain in a rat model.

METHODS:

Experimental diabetes in rats was induced by a single dose of streptozotocin (STZ) administration. The therapeutic efficiency of Epalrestat nanoparticles (0.25, 0.50, 1, and 5 mg/kg) in diabetic rats was studied. STZinduced diabetic rats were treated with different doses of E-SLN for 8 weeks. The nanoparticles were orally administered at a single dose in rats, and the various parameters related to peripheral neuropathy were evaluated and compared with the bare drug. The blood glucose level was estimated by standard glucometer, HbA1c, triglycerides, total cholesterol, and liver function test (ALT and AST) were analyzed by blood samples collected from retro-orbital plexus. Oxidative stress markers and Na+K+ATPase, TNF-α, and IL-1ß levels were measured in the homogenate of sciatic nerves. Behavioral tests were also performed by the hot plate method and tail-flick method.

RESULTS:

E-SLN synthesized by the micro-emulsification method was 281 ± 60 nm in size, and encapsulation efficacy was found to be 88 ± 2%. Optimized E-SLN were characterized and found to be optimum in size, spherical shape, decent encapsulation efficiency, stable at acidic gastric pH, and suitable for oral delivery. E-SLNs did not significantly reverse the STZ-induced elevated blood glucose level (FBS and PPBS), HbA1c, triglycerides, and total cholesterol but significantly improved TNF-α, IL-1ß, and increased Na+K+ATPase levels, oxidative stress marker and ALT, AST in the treated rat group as compared with the diabetic group. Doses of E-SLN, i.e. 0.5, 1.0, 2.5, and 5 mg/kg, significantly increased the tail-flick latency time and hot plate response time in a dose-dependent manner compared with the diabetic group.

CONCLUSION:

Thus, it is suggested that E-SLN were equally effective and less hepatotoxic compared with the standard treatment of epalrestat. To the best of our knowledge, we, for the first time, propose the orally deliverable E-SLN that ameliorates STZ-induced diabetes neuropathic pain effectively as compared with conventional epalrestat.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Diabetes Mellitus Experimental / Neuropatías Diabéticas / Neuralgia Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: Curr Drug Metab Asunto de la revista: METABOLISMO / QUIMICA Año: 2022 Tipo del documento: Article País de afiliación: India

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Diabetes Mellitus Experimental / Neuropatías Diabéticas / Neuralgia Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: Curr Drug Metab Asunto de la revista: METABOLISMO / QUIMICA Año: 2022 Tipo del documento: Article País de afiliación: India
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