Preparation, characterization and in-vivo evaluation of microemulsions containing tamoxifen citrate anti-cancer drug.
The aim of this study was to prepare and characterize a new nanocarrier for oral delivery of tamoxifen citrate (TMC) as a lipophilic oral administrated drug. This drug has low oral bioavailability due to its low aqueous solubility. To enhance the solubility of this drug, the microemulsion system was applied in form of oil-in-water. Sesame oil and Tween 80 were used as drug solvent oil and surfactant, respectively. Two different formulations were prepared for this purpose. The first formulation contained edible glycerin as co-surfactant and the second formulation contained Span 80 as a mixed surfactant. The results of characterization showed that the mean droplet size of drug-free samples was in the range of 16.64-64.62nm with a PDI value of <0.5. In a period of 6months after the preparation of samples, no phase sedimentation was observed, which confirmed the high stability of samples. TMC with a mass ratio of 1% was loaded in the selected samples. No significant size enlargement and drug precipitation were observed 6months after drug loading. In addition, the drug release profile at experimental environments in buffers with pH=7.4 and 5.5 showed that in the first 24h, 85.79 and 100% of the drug were released through the first formulation and 76.63 and 66.42% through the second formulation, respectively. The in-vivo results in BALB/c female mice showed that taking microemulsion form of drug caused a significant reduction in the growth rate of cancerous tumor and weight loss of the mice compared to the consumption of commercial drug tablets. The results confirmed that the new formulation of TMC could be useful for breast cancer treatment.
Chemical Engineering Department, Faculty of Engineering, Ferdowsi University of Mashhad, Mashhad, P. O. Box 91779-48974, Islamic Republic of Iran.
Faranak
F
Dehghani
Chemical Engineering Department, Faculty of Engineering, Ferdowsi University of Mashhad, Mashhad, P. O. Box 91779-48974, Islamic Republic of Iran. Electronic address: n.farhadian@um.ac.ir.
Nafiseh
N
Farhadian
Pharmacy Department, Mashhad University of Medical Sciences, Mashhad, P.O. Box: 91388-13944, Islamic Republic of Iran.
Shiva
S
Golmohammadzadeh
Chemical Engineering Department, Faculty of Engineering, Ferdowsi University of Mashhad, Mashhad, P. O. Box 91779-48974, Islamic Republic of Iran.
Amir
A
Biriaee
Faculty of Medicine, Mashhad University of Medical Sciences, Mashhad, P.O. Box: 91388-13944, Islamic Republic of Iran.
Mahmoud
M
Ebrahimi
Faculty of Medicine, Mashhad University of Medical Sciences, Mashhad, P.O. Box: 91388-13944, Islamic Republic of Iran.
Mohammad
M
Karimi
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000378:metabolism; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000008:administration & dosage / Q000138:chemical synthesis / Q000378:metabolism; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004655:Emulsions; D005260:Female; D051379:Mice; D008807:Mice, Inbred BALB C; D058726:Nanoconjugates / Q000008:administration & dosage; D013120:Spinal Cord Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D013629:Tamoxifen / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000378:metabolism; D047368:Tumor Burden / Q000187:drug effects / Q000502:physiology
D000970:Antineoplastic Agents; D004337:Drug Carriers; D004655:Emulsions; D058726:Nanoconjugates; D013629:Tamoxifen
Breast cancer; In-vitro drug release; In-vivo performance; Microemulsion; Tamoxifen citrate