Formulation and Evaluation of Lyophilized Nanocochleates of Paclitaxel – For Cancer Chemotherapy

Abstract

The nanocochleates are mainly prepared from the liposomes of active pharmaceutical ingredients (APIs) with the help of inactive ingredients like phosphatidylserine (PS) and calcium. The PS shows a considerable binding affinity towards calcium mainly due to the calcium’s tendency to lose part of its hydration shell and to displace water upon complexation. Due to neutralization of the electrostatic charge, calcium causes aggregation & fusion of liposomes composed PS with each other. It has been reported that ca⁺⁺ has an affinity to form a more tightly packed & highly ordered and less hydrated structure than mg⁺⁺ with phosphatidylserine, even at a much lower concentration. It is well documented that ca⁺⁺ plays a vital role in natural membrane fusion phenomena while other cations are ineffective in most such systems. The stability of Nano-cochleate can be increased by doing freeze-drying of finished product which in turn provides a longer shelf life to the product at, where solution form is most unstable. Based on various literature survey and laboratory work, ‘The Ethanol Injection Method’ was selected for the preparation of Nanoliposomes followed by Nanocochleates. The developed Nanocochleates exhibited higher encapsulation efficiency and controlled release of Paclitaxel. This technology may bring about a reduction in dose as well as cost and increase patient compliance. These Nanocochleates could therefore advantageously be employed to improve anticancer activity of Paclitaxel and an alternative to present intravenous administration. From the present study, it can be concluded that the developed Nanocochleates exhibited higher encapsulation efficiency and controlled release of Paclitaxel which may prove to be a suitable & potential candidate for healing a Cancer at a lower concentration.