The preparation of lipid-based drug delivery system using melt extrusion

Chauhan, Gautam; Kulkarni, Nishant S.; Gupta, Vivek

doi:10.1016/j.drudis.2020.07.025

Cited by 16 publications

(4 citation statements)

References 139 publications

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“…In this study, we prepared an inhaled erlotinib nanoemulsion formulation using hot melt extrusion, a continuous manufacturing technique which can be easily scaled up to large scale production in pharmaceutical industry. While a few studies were reported for preparing lipid-based formulations using hot melt extrusion, most of them usually require an additional size reduction step, such as high-pressure homogenization or sonication [ 19 , 30 ]. In our study, we were able to prepare lipid-based nanoemulsions using HME without any additional steps using super refined grade excipients provided by CRODA Inc.…”

Section: Discussionmentioning

confidence: 99%

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Scalable Production and In Vitro Efficacy of Inhaled Erlotinib Nanoemulsion for Enhanced Efficacy in Non-Small Cell Lung Cancer (NSCLC)

et al. 2023

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Non-small cell lung cancer (NSCLC) is a global concern as one of the leading causes of cancer deaths. The treatment options for NSCLC are limited to systemic chemotherapy, administered either orally or intravenously, with no local chemotherapies to target NSCLC. In this study, we have prepared nanoemulsions of tyrosine kinase inhibitor (TKI), erlotinib, using the single step, continuous manufacturing, and easily scalable hot melt extrusion (HME) technique without additional size reduction step. The formulated nanoemulsions were optimized and evaluated for their physiochemical properties, in vitro aerosol deposition behavior, and therapeutic activity against NSCLC cell lines both in vitro and ex vivo. The optimized nanoemulsion showed suitable aerosolization characteristics for deep lung deposition. The in vitro anti-cancer activity was tested against the NSCLC A549 cell line which exhibited 2.8-fold lower IC50 for erlotinib-loaded nanoemulsion, as compared to erlotinib-free solution. Furthermore, ex vivo studies using a 3D spheroid model also revealed higher efficacy of erlotinib-loaded nanoemulsion against NSCLC. Hence, inhalable nanoemulsion can be considered as a potential therapeutic approach for the local lung delivery of erlotinib to NSCLC.

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Section: Discussionmentioning

confidence: 99%

“…Hot melt extrusion (HME) is a continuous manufacturing technique which has been used to prepare numerous FDA-approved products on the market [ 19 ]. In this technique, the material is passed through an extruder under high shear and temperature to give a homogenously dispersed product.…”

Section: Introductionmentioning

confidence: 99%

Scalable Production and In Vitro Efficacy of Inhaled Erlotinib Nanoemulsion for Enhanced Efficacy in Non-Small Cell Lung Cancer (NSCLC)

et al. 2023

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“…To make sure that we preserved the drug's crystallinity, we preferred to process at the lowest processing condition. A lipid can be used as a processing aid, and it is an alternative to a chemical plasticizer [22]. Here, the lipid did not undergo to any chemical degradation such as acid hydrolysis when extruding at higher temperature [23].…”

Section: Hme Processing Methods and Carriers Screening Studiesmentioning

confidence: 99%

Development and Characterization of Sustained-Released Donepezil Hydrochloride Solid Dispersions Using Hot Melt Extrusion Technology

et al. 2021

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The aim of this work was to develop the sustained release formulation of donepezil hydrochloride (DH) using the hot-melt extruded solid dispersion technique via the rational screening of hydrophobic carriers. Hydrophobic carriers with different physicochemical properties such as pH-independent swellability, low-permeability (Eudragit® RS PO (E-RS)), pH-independent non-swellability (ethyl cellulose N7 (EC-N7)), and the presence of lipids (Compritol® 888 ATO (C-888)) with or without pore-forming agents were used to achieve the sustained release profile of DH. Mannitol (MNT) was chosen as the temporary pore-forming agent. The thermal analysis showed that both the drug and C-888 preserved their crystallinity within a solid dispersion. During a dissolution test, MNT could generate pores, and the drug release rate was proportionally correlated to the MNT content. Tailoring of the ratio of C-888 and MNT in the formulations along with an appropriate extrusion temperature profile resulted in the modified release of DH, and a preferable release pattern was obtained under these conditions. C-888 was chosen for the further investigations to obtain tablets with a high integrity. The optimized tablets were compared to the marketed formulation of Aricept® in terms of drug release profiles. The optimized formulation showed the stable and sustained release behavior of extended release profile, which was close to the release behavior of Aricept® with good tablet characteristics. It was concluded that the hot-melt extrusion technique can be utilized for the manufacturing of DH sustained release tablets with improved tablet integrity and characteristics by co-processing the tablet excipient with DH/C-888.

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“…High biocompatibility [ 2 ], unique adsorption properties [ 3 , 4 ], and large surface area of graphene allow it to form a compatible interface with phospholipid molecules [ 5 , 6 , 7 , 8 ]. Both graphene and phospholipids separately are widely used in biosensing [ 9 , 10 , 11 , 12 , 13 ] and drug delivery [ 14 , 15 , 16 ]. It is predicted that the synergistic effect of graphene and phospholipids could be used in various biomedical devices [ 17 , 18 , 19 , 20 , 21 ].…”

Section: Introductionmentioning

confidence: 99%

Nanoindentation of Graphene/Phospholipid Nanocomposite: A Molecular Dynamics Study

Shunaev

Glukhova

2021

Molecules

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Graphene and phospholipids are widely used in biosensing and drug delivery. This paper studies the mechanical and electronic properties of a composite based on two graphene flakes and dipalmitoylphosphatidylcholine (DPPC) phospholipid molecules located between them via combination of various mathematical modeling methods. Molecular dynamics simulation showed that an adhesion between bilayer graphene and DPCC increases during nanoindentation of the composite by a carbon nanotube (CNT). Herewith, the DPPC molecule located under a nanotip takes the form of graphene and is not destroyed. By the Mulliken procedure, it was shown that the phospholipid molecules act as a “buffer” of charge between two graphene sheets and CNT. The highest values of electron transfer in the graphene/DPPC system were observed at the lower indentation point, when the deflection reached its maximum value.

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The preparation of lipid-based drug delivery system using melt extrusion

Cited by 16 publications

References 139 publications

Scalable Production and In Vitro Efficacy of Inhaled Erlotinib Nanoemulsion for Enhanced Efficacy in Non-Small Cell Lung Cancer (NSCLC)

Scalable Production and In Vitro Efficacy of Inhaled Erlotinib Nanoemulsion for Enhanced Efficacy in Non-Small Cell Lung Cancer (NSCLC)

Development and Characterization of Sustained-Released Donepezil Hydrochloride Solid Dispersions Using Hot Melt Extrusion Technology

Nanoindentation of Graphene/Phospholipid Nanocomposite: A Molecular Dynamics Study

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