Formulation of Lyophilized, Stable Nanocochleates of Docetaxel: Design, Optimization, and Characterization

Asian Journal of Pharmaceutical Technology and Innovation (ajpti)

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Commentary- Asian Journal of Pharmaceutical Technology and Innovation(2021)

Formulation of Lyophilized, Stable Nanocochleates of Docetaxel: Design, Optimization, and Characterization

Mallappa S Harwalkar*
Department of Specialized Veterinary Sciences, Islamic Azad University, Sciences and Research Branch, Iran
*Corresponding Author:
Mallappa S Harwalkar, Department of Specialized Veterinary Sciences, Islamic Azad University, Sciences and Research Branch, Iran, Email:

Received: 01-Oct-2021 Accepted Date: Oct 22, 2021 ; Published: 30-Oct-2021


Liposomes were discovered by Alec D Bangham during the 1960s at the Babraham Institute, University of Cambridge, and comprise of single or different concentric lipid bilayers encapsulating an aqueous compartment. The first formulation was made natural lipids; at present they can incorporate regular and additionally manufactured lipids and surfactants. They have the capacity of ensnaring both lipophilic and hydrophilic agent, in the lipid layer and in the aqueous core, respectively. The size of these almost circular lipid vesicles can range from a couple of nanometers to a few micrometers. However, liposomes applied to medical use range between 50 and 450 nm. Liposomes appear to be a practically perfect drug-carrier system, since their morphology is like that of cellular membranes and on account of their capacity to consolidate different substances. Thusly, throughout the previous 50 years liposomes have been broadly examined and they keep on being the subject of extraordinary research. They are esteemed for their natural and technological advantages delivery systems for biologically active substances, both in vitro and invitro, and are viewed as the best drug-carrier system known to date. During the two a decades ago, outstanding advancement has been made, and a few biomedical uses of liposomes are either in clinical trials or are going to be put available, while others have just been approved for public use.

Pre-formulation Study

Pre formulation study is desired to ensure the development of a stable as well as the therapeutically effective and safe dosage form. Pre formulation testing is designed to assess the influence of physicochemical properties of drug substances and excipients on formulation properties of dosage form, technique for fabricate and pharmacokinetic biopharmaceutical properties of the subsequent product. An intensive comprehension of physicochemical properties may eventually confirm that no significant hindrances are present for the formulation development.

Formulation and Development

Characterization of drug is necessary because to identify particular drug, and to check the purity of drug, to determine physicochemical properties which help for development of particular dosage form. Docetaxel sample was characterized by identification test, solubility study, melting point, UV analysis, FT-IR analysis. Melting point is utilized for assurance of purity and identification of drug. The melting point of Docetaxel was determined by melting point apparatus utilizing capillary method.

Fine powder of Atorvastatin calcium was filled in glass capillary tube which was recently fixed toward one side. The capillary tube was tied with thermometer and afterward immersed into melting point apparatus. The temperature was seen at which drug started to melt by thermometer which was already dip into the liquid paraffin apparatus. Liposome offers many advantages over conventional dosage forms, like increased bioavailability, possibility of releasing drug at slower and constant rate, accurate drug release. Docetaxel is approved by the FDA for treatment of locally advanced or metastatic breast cancer, head and neck cancer, gastric cancer. Docetaxel is BCS Class 4 drug; hence efficacy can be improved with liposomal formulation. Docetaxel anhydrous is insoluble in water with Partition coefficient (log P=2.4). Considering all above parameter Docetaxel was selected as model drug candidate for increasing its water permeability and bioavailability through liposome formulation. As part of Pre-formulation studies, solubility of drug in various organic solvent and water, melting point was determined to enable selection of excipients with good drug loading ability. Selected lipid (HSPC), sterol (cholesterol), and release modifier (DPPE: PEG-2000), were tried in different proportions for liposome. Formulation batches were designed on the basis of solvent, lipid to cholesterol ratio, lipid to release modifier ratio, hydration temperature etc. Formulations were optimised on three test i.e. homogeneous formulation, particle size, zeta potential, entrapment efficiency. Preliminary batch L6 selected as model for design of trail batches. Optimized formulations were further characterized for droplet size measurement, Zeta potential, entrapment efficiency. Batch L1 and L2 having good results. Hence these batches were further subjected to in vitro drug release and assay of the formulation.