TY - JOUR
T1 - Abemaciclib-loaded ethylcellulose based nanosponges for sustained cytotoxicity against MCF-7 and MDA-MB-231 human breast cancer cells lines
AU - Anwer, Md Khalid
AU - Fatima, Farhat
AU - Ahmed, Mohammed Muqtader
AU - Aldawsari, Mohammed F.
AU - Alali, Amer S.
AU - Kalam, Mohd Abul
AU - Alshamsan, Aws
AU - Alkholief, Musaed
AU - Malik, Abdul
AU - Az, Alanazi
AU - Al-shdefat, Ramadan
N1 - Publisher Copyright:
© 2022 The Author(s)
PY - 2022/6
Y1 - 2022/6
N2 - Abemaciclib (AC) is a novel, orally available drug molecule approved for the treatment of breast cancer. Due to its low bioavailability, its administration frequency is two to three times a day that can decrease patient compliance. Sustained release formulation are needed for prolong the action and to reduce the adverse effects. The aim of current study was to develop sustained release NSs of AC. Nanosponges (NSs) was prepared by emulsion-solvent diffusion method using ethyl-cellulose (EC) and Kolliphor P-188 (KP-188) as sustained-release polymer and surfactant, respectively. Effects of varying surfactant concentration and drug: polymer proportions on the particle size (PS), polydispersity index (PDI), zeta potential (ζP), entrapment efficiency (%EE), and drug loading (%DL) were investigated. The results of AC loaded NSs (ACN1-ACN5) exhibited PS (366.3–842.2 nm), PDI (0.448–0.853), ζP (−8.21 to −19.7 mV), %EE (48.45–79.36%) and %DL (7.69–19.17%), respectively. Moreover, ACN2 showed sustained release of Abemaciclib (77.12 ± 2.54%) in 24 h Higuchi matrix as best fit kinetics model. MTT assay signified ACN2 as potentials cytotoxic nanocarrier against MCF-7 and MDA-MB-231 human breast cancer cells. Further, ACN2 displayed drug release property without variation in the % release after exposing the product at 25 °C, 5 °C, and 45 °C storage conditions for six months. This investigation proved that the developed NSs would be an efficient carrier to sustain the release of AC in order to improve efficacy against breast cancer.
AB - Abemaciclib (AC) is a novel, orally available drug molecule approved for the treatment of breast cancer. Due to its low bioavailability, its administration frequency is two to three times a day that can decrease patient compliance. Sustained release formulation are needed for prolong the action and to reduce the adverse effects. The aim of current study was to develop sustained release NSs of AC. Nanosponges (NSs) was prepared by emulsion-solvent diffusion method using ethyl-cellulose (EC) and Kolliphor P-188 (KP-188) as sustained-release polymer and surfactant, respectively. Effects of varying surfactant concentration and drug: polymer proportions on the particle size (PS), polydispersity index (PDI), zeta potential (ζP), entrapment efficiency (%EE), and drug loading (%DL) were investigated. The results of AC loaded NSs (ACN1-ACN5) exhibited PS (366.3–842.2 nm), PDI (0.448–0.853), ζP (−8.21 to −19.7 mV), %EE (48.45–79.36%) and %DL (7.69–19.17%), respectively. Moreover, ACN2 showed sustained release of Abemaciclib (77.12 ± 2.54%) in 24 h Higuchi matrix as best fit kinetics model. MTT assay signified ACN2 as potentials cytotoxic nanocarrier against MCF-7 and MDA-MB-231 human breast cancer cells. Further, ACN2 displayed drug release property without variation in the % release after exposing the product at 25 °C, 5 °C, and 45 °C storage conditions for six months. This investigation proved that the developed NSs would be an efficient carrier to sustain the release of AC in order to improve efficacy against breast cancer.
KW - Abemaciclib
KW - Biocompatibility
KW - Cytotoxicity
KW - Ethylcellulose
KW - Nanosponges
UR - http://www.scopus.com/inward/record.url?scp=85128236218&partnerID=8YFLogxK
U2 - 10.1016/j.jsps.2022.03.019
DO - 10.1016/j.jsps.2022.03.019
M3 - Article
AN - SCOPUS:85128236218
SN - 1319-0164
VL - 30
SP - 726
EP - 734
JO - Saudi Pharmaceutical Journal
JF - Saudi Pharmaceutical Journal
IS - 6
ER -