Abstract

Anastrozole (ANZ) is considered constitute of the fourth –generation of Non–steroidal aromatase blockage, ANZ has use for hormone receptor positive breast cancer in postmenopausal women. The serious side effects of ANZ including, vaginal dryness, hot flashes, irritability, breast tenderness and un–stability in circulation.
 Nanostructured lipid carriers (NLCs) have recently emerged as a multifunctional platform for drug delivery in cancer therapy.
 Five formula were composed of (200 mg of glyceryl monostearate, 40 mg of oleic acid , 1% (w/w) Tween 80, 1% (w/w) Poloxamer 407, 1% (w/w) soy lecithin and Vitamin E Polyethylene Glycol Succinate.
 The mean particle size, polydispersity index, zeta potential, entrapment efficiency, loading capacity range of optimum formula F05 (166±3.86 nm), (0.271±0.04), (–23.7±2.65 mV), (42.43±3.90%) and (1.23±0.35%) respectively that prepared by same above composition but higher amplitude value (70%). The in–vitro drug leakage study demonstrated intact formula through 5 hours, with an approximately 78.37% of the drug was encapsulated, that exhibit an anomalous release mechanism.

Highlights

  • Due to patient preference, lower costs, proven effectiveness, lack of infusion-related discrepancies, and the opportunity of developing chronic treatment regimes, the use of oral anticancer drugs has increased during the last decade

  • Materials The following material were utilized in the present study with their suppliers: ANZ, Glyceryl monostearate (GMS), oleic acid (OA), Poloxamer 407 (P407),Vitamin E Polyethylene Glycol Succinate (E–TPGS), Lecithin from Soybean, Tween®80 and Cetyl palmitate (HyperChem®, Zhejiang, China)

  • (28±4.31 mg/g) in glyceryl monostearate (GMS) compared to other lipids being investigated as seen in figure (1)

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Summary

Introduction

Lower costs, proven effectiveness, lack of infusion-related discrepancies, and the opportunity of developing chronic treatment regimes, the use of oral anticancer drugs has increased during the last decade. The first factor that can increase dissolution and absorption is pharmaceutical modification or the physicochemical characteristics of the drug. Anastrozole (ANZ) is a nonsteroidal benzyltriazole with molecular formula:. ANZ is structurally related to letrozole, fadrozole and vorozole, with all being classified as azoles(2) .It is class III as BCS (high solubility with low permeability) (3). Molecular weight: 293.37 Da. Density:1.08 g/cm[3]. Solubility: very slightly soluble in water (0.53 mg/ml at 25 °C); freely soluble in alcohol, methyl alcohol, acetone and in tetrahydrofuran, very soluble in acetonitrile(5). The log P (octanol/water) is 1.58 , indicating that it is a moderately lipophilic compound(6)

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