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Evaluation and optimization of pH-responsive niosomes as a carrier for efficient treatment of breast cancer

  • Salem, Heba F.1
  • Kharshoum, Rasha M.1
  • Abo El-Ela, Fatma I.2
  • F, Amr Gamal1
  • Abdellatif, Khaled R. A.3, 4
  • 1 Beni-Suef University, Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, El-Shahid/Shehata Ahmed Hijaz St., Beni-Suef, Egypt , Beni-Suef (Egypt)
  • 2 Beni-Suef University, Department of Pharmacology, Faculty of Veterinary Medicine, Beni-Suef, Egypt , Beni-Suef (Egypt)
  • 3 Beni-Suef University, Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Beni-Suef, Egypt , Beni-Suef (Egypt)
  • 4 Ibn Sina National College for Medical Studies, Pharmaceutical Sciences Department, Jeddah, 21418, Kingdom of Saudi Arabia , Jeddah (Saudi Arabia)
Published Article
Drug Delivery and Translational Research
Springer US
Publication Date
Feb 27, 2018
DOI: 10.1007/s13346-018-0499-3
Springer Nature


Tamoxifen citrate (TXC) is commonly indicated to prevent cell multiplication and development of breast cancer. However, it is usually associated with limited activity and development of toxicity and resistance. This study aimed to describe an in situ pH-responsive niosomes as a carrier for localized and sustained delivery of TXC. The thin film hydration method was utilized to produce TXC niosomes using sorbitan monostearate and cholesterol of 1:1 Molar ratio. The produced formula displayed nano-spherical shape with entrapment efficiency (EE) of 88.90 ± 0.72% and drug release of 49.2 ± 1.51% within 8 h. This formula was incorporated into chitosan/glyceryl monooleate (CH/GMO) as a localized in situ pH-responsive hydrogel delivery system. Different formulae were produced by Design-Expert software based on user-defined response surface design utilizing different chitosan concentration (A) and GMO concentration (B) characterized for mean viscosity (R2) and in vitro release studies (R1). The results displayed that R1 was significantly antagonistic with both of A and B while R2 was significantly synergistic with both of them. The optimum formula was selected and capped with gold as an ideal candidate for computed tomography (CT) to evaluate the efficacy and tissue distribution of TXC utilizing Ehrlich carcinoma mice model. The optimum formula showed localized TXC in a tumour and consequently a significant anti-tumour efficacy compared with free TXC. Based on these outcomes, the novel in situ pH-responsive TXC-loaded noisome could be a promising formula for the efficient treatment of breast cancer.

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