TY - JOUR
T1 - Preparation, evaluation and pharmacokinetic studies of spray dried PLGA polymeric submicron particles of simvastatin for the effective treatment of breast cancer
AU - Anzar, Naqueeb
AU - Mirza, Mohd Aamir
AU - Anwer, Khalid
AU - Khuroo, Tahir
AU - Alshetaili, Abdullah S.
AU - Alshahrani, Saad M.
AU - Meena, Jairam
AU - Hasan, Nazia
AU - Talegaonkar, Sushama
AU - Panda, Amulya K.
AU - Iqbal, Zeenat
N1 - Publisher Copyright:
© 2017
PY - 2018/1
Y1 - 2018/1
N2 - In the current study, simvastatin-loaded PLGA submicron particles (SIM SP) were prepared by the spray drying method. Different parameters of the nanospray drying method, such as the inlet temperature, spray mesh diameter, the spray rate, and the gas flow rate, were optimized and a particle of size 259.1 nm was obtained, utilizing a 7 μm mesh sieve. Percent drug entrapment efficiency and drug loading capacity were calculated as 63.07% and 85.23 μg/mg, respectively. A 66.61% cumulative drug release was recorded after 72 h, in accordance to the Higuchi diffusion pattern followed by Fickian transport. An amorphous form drug was entrapped inside the polymer, and no interaction of the drug with the polymer was observed. An MTT assay was conducted in the MCF-7 cell lines to search for anti-cancerous activity. The pharmacokinetic studies clearly demonstrated that SIM SP exhibited significant increase in AUC0–24, T1/2 and Cmax and decrease in Kel, compared to pure SIM. Therefore, it can be concluded that submicronic particles acquired by nanospray drying were found to be appropriate for the treatment of solid tumor.
AB - In the current study, simvastatin-loaded PLGA submicron particles (SIM SP) were prepared by the spray drying method. Different parameters of the nanospray drying method, such as the inlet temperature, spray mesh diameter, the spray rate, and the gas flow rate, were optimized and a particle of size 259.1 nm was obtained, utilizing a 7 μm mesh sieve. Percent drug entrapment efficiency and drug loading capacity were calculated as 63.07% and 85.23 μg/mg, respectively. A 66.61% cumulative drug release was recorded after 72 h, in accordance to the Higuchi diffusion pattern followed by Fickian transport. An amorphous form drug was entrapped inside the polymer, and no interaction of the drug with the polymer was observed. An MTT assay was conducted in the MCF-7 cell lines to search for anti-cancerous activity. The pharmacokinetic studies clearly demonstrated that SIM SP exhibited significant increase in AUC0–24, T1/2 and Cmax and decrease in Kel, compared to pure SIM. Therefore, it can be concluded that submicronic particles acquired by nanospray drying were found to be appropriate for the treatment of solid tumor.
KW - MCF-7
KW - MTT assay
KW - Nanospray dryer
KW - Simvastatin
KW - Solid tumor
UR - http://www.scopus.com/inward/record.url?scp=85034865372&partnerID=8YFLogxK
U2 - 10.1016/j.molliq.2017.11.081
DO - 10.1016/j.molliq.2017.11.081
M3 - Article
AN - SCOPUS:85034865372
SN - 0167-7322
VL - 249
SP - 609
EP - 616
JO - Journal of Molecular Liquids
JF - Journal of Molecular Liquids
ER -