Optimization Studies on Imatinib Mesylate Loaded Nanoliposomes Using Box-Behnken Design

Mandeep Dahiya, Rajendra Awasthi, Gaurav Gupta, Sachin Kumar Singh, Monica Gulati, Niraj Kumar Jha, Saurabh Kumar Jha, Ankur Sharma, Parteek Prasher, Krishnan Anand, Dinesh Kumar Chellappan, Kamal Dua, Harish Dureja

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Abstract

Nanoliposomes are bilayer phospholipid vesicles used to encapsulate and deliver therapeutic agents. The study was aimed to investigate the effects of critical variables on nanoliposomes characteristics. Imatinib mesylate-loaded nanoliposomes were formulated by the two-step emulsification process using a high-speed homogenizer system and probe-type ultrasonicator. The Box-Behnken design was utilized to optimize the process parameters. The mean particle size of nanoliposomes was found to be 211 nm to 623.3 nm with a low value of polydispersity index (0.005 to 0.7). Zeta potential values varied from -27.6 mV to -9.2 mV in uncoated nanoliposomes to +27.5 mV in chitosan-coated nanoliposomes. The encapsulation efficiency in formulation NLP-H8 containing 200 mg of phosphatidylcholine, homogenization speed of 12000 rpm, and 7 min of sonication time was found to be 76.49% without the coating and 85.4% in 0.2% w/v chitosan-coated nanoliposomes. TEM image confirmed the spherical shape of nanoliposomes. In-vitro drug release study demonstrated that the optimized nanoliposomal formulations released 84.67% of the loaded drug after 24h in 0.1N HCl. The IC50 value of formulation NLP-H8 was found to be 7.98 μM. Nanoliposomal formulations were prepared successfully with suitable size, morphology, encapsulation efficiency, and drug release. The models developed in this study may be utilized further as a response surface for the various parameters of nanoliposomes.

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Nano Biomedicine and Engineering.

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