Publications on lipid-based formulations
Oxidative Stability in Lipid Formulations: a Review of the Mechanisms, Drivers, and Inhibitors of Oxidation
Jasmine Musakhanian, Jean-David Rodier and Masumi Dave
Cannabinoid molecules and their love of lipid excipients
Gattefossé
Carving out a Niche in Pharmaceutical Drug Delivery
Ketkee Deshmukh, Agnivesh Shrivastava, Sunil Bambarkar
Pharma Times – Vol. 53 – No. 12, December 2021
GELUCIRE® 4414 for type IV lipid based formulations and their in vitro in vivo performance evaluation
AGNIVESH SHRIVASTAVA , KETKEE DESHMUKH, RENUKA TIWARI, SUNIL BAMBARKAR, NABIL FARAH,
KAVITA SINGH
AAPS 2021
In this study, Gelucire® 44/14 in type IV lipid-based formulation has been evaluated to increase the solubility and in vivo performance of ticagrelor.
Lipid excipients to unlock oral bioavailability issues
American Pharmaceutical Review, February 2021
Camille Dumont, Cécile Morin
Introduction
Chapter I : Lipids, reliable partners to enhance oral bioavailability of poorly water-soluble drugs
Chapter II : Lipids to enhance the intestinal permeability of poorly permeable drugs
Chapter III : Targeting lymphatic absorption with appropriate lipid excipients selection
Chapter IV : Mitigating food effect with lipid-based formulations
Chapter V : Gattefossé range of functional excipients
for oral bioavailability enhancement
DOs and DON’Ts for developing successful SEDDS formulations to enhance API bioavailability
Inayet Ellis
Tablets & Capsules, April 2020
Successful oral delivery of poorly water-soluble drugs both depends on the intraluminal behavior of drugs and of appropriate advanced drug delivery systems
Ben J. Boyd, Christel A.S. Bergström, Zahari Vinarov, Martin Kuentz, Joachim Brouwers, Patrick Augustijns, Martin Brandl, Andreas Bernkop-Schnürch, Neha Shrestha, Véronique Préat, Anette Müllertz, Annette Bauer-Brandl, Vincent Jannin
European Journal of Pharmaceutical Sciences, Volume 137, 2019, 104967,
ISSN 0928-0987, https://doi.org/10.1016/j.ejps.2019.104967.
In this excellent review article issued from the UNGAP program (European Network on Understanding Gastro-intestinal Absorption-related Process) you will find relevant and up-to-date information on:
- Poorly water soluble drugs and the link between physico-chemical properties and solubility, lipophilicity and permeability
- Technologies to increase solubility and dissolution rate: salt formation, amorphous solid dispersions, lipid-based formulations
- How to avoid precipitation and create a concentration gradient to improve absorption
- Methods for modelling the performance such as Molecular Dynamics Simulations
- In vitro methods for solubility and dissolution assessments
- Methods to explore the absorption in the GI tract: GI concentration-time profile, in vitro digestion, in vitro models coupling dissolution and permeation, mucus diffusion
- Impact of molecularly dissolved drug versus apparently dissolved drug (ie in colloidal structure)
Amélioration de la biodisponibilité des substances actives via la formulation galénique
[Bioavailability enhancement of active pharmaceutical ingredients through formulation strategies]
E Levacher, C Buffangeix, MJ Celadon, I Decorte, P Gestin, J Hecq, F Jego, B Paillard, A Plantefeve, X Thomas
The SFSTP commission on Bioavailability published an article reviewing the formulation strategies to enhance the bioavailability of APIs.
Interestingly this article is both in French and English languages.
I Introduction
II Prerequisites
1 Initial identification and characterization of the active ingredient
1.1 Physico-chemical characteristics
1.2 Impact of physicochemical characteristics on absorption
1.3 Passive diffusion prediction tools
1.4 In silico prediction
2 Biopharmaceutical classifications
III Formulation strategies
1 prerequisites
2 techniques for increasing the dissolution rate
3 Solubility enhancement technologies
4 Improving the permeability, oral route
IV Control, assessment, prediction of the bioavailability
1 Physicochemical control methods for the manufacturing intermediates and finished products
2 Assessing an dpredicting the bioavailability of the formulations
V Alternative strategy: changing the route of administration
VI Conclusion: decision tree
Lipid based delivery system
Pharma Times September 2019 – Special issue
Lipid excipients in pharmaceutical technologies
Nabil FARAH and Joel DENIS
Lipidic excipients in drug delivery for solubility and bioavailability enhancement
Prashantkumar K. PARMAR, Srilaxmi G. RAO, Arvind KK. BANSAL
From exploration of lipids to its exploitation in market: Pharmaceuticals, Nutraceuticals and Herbal
Saurabh ARORA, Abhinav GARG, Karishma KAPOOR
A snapshot of lipid excipients for topical formulations
Renuka TIWARI, Ketkee DESHMUKH, Agnivesh SHRIVASTAVA, Kanchan KOHLI
Strategic lipid-based delivery interventions for enhancing oral bioavailability of BCS II/IV drugs
Teenu SHARMA, Ranjot KAUR, Sumant SAINI, Atul JAIN, Bhupinder SINGH
Unleashing role of excipients in overcoming formulation challenges
Meenakshi VENKATARAMAN, Megha MARWAH, Mangal NAGARSENKER
Role of lipid excipients in oral sustained release drug delivery systems
Divya JAIN, Namita DESAI
Understanding The Role Of In Vitro And In Vivo Evaluation Techniques In Determining the Performance of Lipid-Based Formulations
Ketkee DESHMUKH, Agnivesh SHRIVASTAVA, Sunil BAMBARKAR, Nabil FARAH, Kavita SINGH
In this case study using curcuminoids as model drug, the authors show that in vitro lipolysis test is a useful tool to predict in vivo performance
Poster CRS 2019
Colloidal aspects of dispersion and digestion of self-dispersing lipid-based formulations for poorly water-soluble drugs
Kapilkumar Vithani, Vincent Jannin, Colin W. Pouton, Ben J. Boyd
In this review article, the authors explain the importance of the colloidal structures formed during dispersion and digestion of self emulsifying lipid-based formulations on drug solubilization and absorption.
A review of the techniques used to characterize the colloidal structures is also carried out.
Complex Interplay between Solubilization, Digestion, Supersaturation and Absorption of Poorly Soluble Drugs with Lipid-Based Formulations
LIPID-BASED DELIVERY – Are Lipid-Based Drug Delivery Systems in Your Formulation Toolbox?
Dr. Jason LePree Drug Development & Delivery, Issue: October 2017, Posted Date: 9/29/2017 This article reviews the causes of poor bioavailability for drugs. It provides an introduction to lipid-based drug delivery systems, and how the formulation approach can be used to overcome impediments to good bioavailability of therapeutic actives, including poor water solubility, low permeability, and degradation by stomach acid or enzymes in vivo.
Reaching milestones in lipid-based formulations: from effective prediction to successful development
September 2015 This white paper describes the important milestones achieved in lipid based formulation (LBF) development for oral drug delivery. Collaborative research between academic and industrial partners has increased understanding of the functional properties of lipid excipients and the role they play in solubilizing poorly water soluble compounds. It has also led to the development of in vitro – in vivo predictive analytical tools. The key scientific articles describing these milestones are collected in this one White Paper, providing a single source of practical information for those interested in lipid formulation development.
Development of self emulsifying lipid formulations of BCS class II drugs with low to medium lipophilicity
Vincent Jannin, Stéphanie Chevrier, Matthieu Michenaud, Camille Dumont, Silvia Belotti, Yann Chavant, Fédéric Demarne.
This acticle describes the work undertaken in Gattefossé R&D labs (St Priest) to develop lipid formulations for low to medium lipophilicity API: piroxicam, nifedipine and curcurmin and evaluate the effect of in-vitro digestion on the solubilizing capacity of the formulations.
Formulation of a self-emulsifying lipid formulation of curcumin
Vincent Jannin, Camille Dumont, Hamza Benhaddou, Stéphanie Chevrier, Yann Chavant, Christophe Voutsinas, Frédéric Demarne
AAPS 2014
