SOME MULTIFUNCTIONAL LIPID EXCIPIENTS AND THEIR PHARMACEUTICAL APPLICATIONS
DOI:
https://doi.org/10.22159/ijpps.2019v11i9.34194Keywords:
Bioavailability, Lipid Based Drug Delivery System, ExcipientsAbstract
This review is generally focussed on lipid-based excipients in solid oral formulations which increase its bioavailability. Several approaches have been used to deliver the drug efficiently in the body, and lipid excipients are one of the promising drug delivery systems which address challenges like solubility and bioavailability of water-soluble drugs. Lipids excipients can be tailored to meet a wide range of product requirements like disease indication, route of administration, stability, toxicity, and efficacy. This review discusses novel lipids like Compritol 888 ATO, Dynasan 114, and Precirol ATO 5 and how these can be employed for devicing efficient drug delivery models and thereby have used in cosmetic and pharmaceutical industries.
Downloads
References
Chapman KD, Dyer JM, Mullen RT. Biogenesis and functions of lipid droplets in plants, thematic review series lipid droplet synthesis and metabolism from yeast to man. J Lipid Res 2012;53:215–26.
A Report by Buddhist Chi Hong Chi Memorial College A. L. Bio Notes (by Denise Wong) The Cell. Enzymes; 2013. p. 49-50.
Sinha V, Rachna K. Polysaccharides in colon-specific drug delivery. Int J Pharm 2001;224:19-38.
Venkata R. Chemical and biological aspects of selected polysaccharides. Indian J Pharm Sci 1992;54:90-7.
Schwartz JB, Simonelli AP, Higuchi WI. Drug release from wax matrices I. Analysis of data with first-order kinetics and with the diffusion-controlled model. J Pharm Sci 1968;57 Suppl 2:274–7.
Lantz RJ, Robinson MJ. Method of preparing sustained release pellets and products thereof; 1964.
Porter CJ, Trevaskis NL, Charman WN. Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs. Nat Rev Drug Discovery 2007;6 Suppl 3:231–48.
Sohi H, Sultana Y, Khar RK. Taste masking technologies in oral pharmaceuticals: recent developments and approaches. Drug Dev Ind Pharm 2004;30 Suppl 5:429–48.
Dubey R, Shami TC, Bhasker Rao KU. Microencapsulation technology and applications. Def Sci J 2009;59 Suppl 1:82–95.
Singh MN, Hemant KSY, Ram M, Shivakumar HG. Microencapsulation: a promising technique for controlled drug delivery. Res Pharm Sci 2010;5 Suppl 2:65–77.
https://www.rose-hulman.edu/brandt/Chem330/lipid properties. [Last accessed on 05 Apr 2019]
Jannin V, Musakhanian J, Marchaud D. Approaches for the development of solid and semi-solid lipid-based formulations. Adv Drug Delivery Rev 2008;60 Suppl 6:734–46.
Ako H, Okuda D, Gray D. Healthful new oil from macadamia nuts. Nutrition 1995;11:286-8.
Andersen KE, Nielsen R. Lipstick dermatitis related to castor oil. Contact Dermatitis 1984;11:253-4.
Bleck O, Abeck D, Ring J. Two ceramide subfractions detectable in Cer (AS) position by HPLTC in skin surface lipids of non-lesional skin of atopic eczema. J Invest Derm 1999;113 Suppl 6:894–900.
Bohlinder K, Olsson B. Use and characteristics of a novel lipid particle forming matrix as a drug-carrier system. Eur J Pharma Sci 1994;2 Suppl 4:271–9.
Bonte F, Pinguet P. Thermotropic phase behavior of in vivo extracted human stratum corneum lipids. Lipids 1997;3 Suppl 6:653–60.
Akoh CC, Yee LN. Enzymatic synthesis of position-specific low-calorie structured lipids. J Am Oil Chem Sci 1997;74 Suppl 11:1409-13.
Bell SJ, Bradley D, Forse RA, Bistrain BR. The new dietary fats in health and disease. J Am Diet Assoc 1997;97 Suppl 3:280-6.
Chambrier C, Guiraud M, Gibault JP, Labrosse H, Bouletreau P. Medium and long-chain triacylglycerols in postoperative patients: structured lipids versus a physical mixture. Nutr 1999;15 Suppl 4:274-7.
Pahlsson P. Characterization of galactosyl glycerolipids in the HT29 human colon carcinoma cell line. Arch Biochem Biophys 1998;396:187–98.
Koga Y, Nishihara M, Morii H, Matsushita MA. Other polar lipids of methanogenic bacteria: structures, comparative aspects and biosyntheses. Microbiol Rev 1983;57:164–82.
Pereto J, Garcia PL, Moreira D. Ancestral lipid biosynthesis an early membrane evolution. Tre Bio Chem Sci 2004;29:469–77.
Cronan JE. Bacterial membrane lipids: where do we stand? Annu Rev Microbiol 2003;57:203–24.
Merrill AH, Sandhoff K. In new comprehensive biochemistry: biochemistry of lipids, lipoproteins and membranes. Else Sci New York; 2002. p. 373–407.
Amidon GL, Lennernas H, Shah VP. A theoretical basis for a biopharmaceutical drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharma Res 1995;12:413–9.
http://www.gattefosse.com/node.php?Articleid=172. [Last accessed on 24 Jun 2009].
Barthelemy P, Laforet JP, Farah N, Joachim J. Compritol 888 ATO: an innovative hot-melt coating agent for prolonged-release drug formulations. Eur J Pharm Biopharm 1999;47:87-90.
Faham A, Prinderre P, Farah N, Eichler KD, Kalantzis G, Joachim J. Hot-melt coating technology. I. influence of compritol 888 ATO and granule size on theophylline release. Drug Dev Ind Pharm 2000;26:167-76.
Faham A, Prinderre P, Piccerelle P, Farah N, Joachim J. Hot melt coating technology: influence of compritol 888 ATO and granule size on chloroquine release. Pharmazie 2000;55:444-8.
Hamdani J, Moes AJ, Amighi K. Development and in vitro evaluation of a novel floating multiple unit dosage forms obtained by melt pelletization. Int J Pharm 2006;322:96-103.
Zhang YE, Schwartz JB. Melt granulation and heat treatment for wax matrix-controlled drug release. Drug Dev Ind Pharm 2003;29:131-8.
Freitas C, Muller RH. Correlation between long-term stability of solid lipid nanoparticles (SLN) and crystallinity of the lipid phase. Eur J Pharm Biopharm 1999;47:125-32.
Koo OMY, Varia SA. Case studies with new excipients: development, implementation and regulatory approval. Ther Delivery 2011;2:949-56.
Food and Drug Administration. Guidance for industry: Nonclinical studies for the safety evaluation of pharmaceutical excipients; 2005.
Maniruzzaman M, Slipper IJ, Vithani K, Douroumis D. Sustained release solid lipid matrices processed by hot-melt extrusion (HME). Colloids Surf B Biointerfaces 2013;110:403-10.
Jannin V, Erard BV, Diaye NA. Comparative study of the lubricant performance of Compritol 888 ATO either used by blending or by hot melt coating. Int J Pharm 2003;262:39-45.
Diaye NA, Jannin V, Erard BV. Comparative study of the lubricant performance of compritol HD5 ATO and compritol 888 ATO: effect of polyethylene glycol behenate on lubricant capacity. Int J Pharm 2003;254:263-9.
Jannin V, Cuppok Y. Hot-melt coating with lipid excipients. Int J Pharm 2013;457:480-7.
Hamdani J, Moes AJ, Amighi K. Development and evaluation of prolonged-release pellets obtained by the melt pelletization process. Int J Pharm 2002;45:167-77.
Hamdani J, Moes AJ, Amighi K. Development and in vitro evaluation of a novel floating multiple unit dosage forms obtained by melt pelletization. Int J Pharm 2006;322:96-103.
Nastruzzi C. Lipospheres in drug targets and delivery: approaches, methods and applications. CRC Press: New York; 2005.
Gan L, Gao YP, Zhu CL. Novel pH-sensitive lipid-polymer composite microspheres of 10-hydroxycamptothecin exhibiting colon-specific biodistribution and reduced systemic absorption. J Pharm Sci 2013;102:1752-9.
Cai S, Yang Q, Bagby TR, Forrest ML. Lymphatic drug delivery using engineered liposomes and solid lipid nanoparticles. Adv Drug Delivery Rev 2011;10:901-8.
Saettone MF, Torracca MT, Pagano A. Controlled release of pilocarpine from coated polymeric ophthalmic inserts prepared by hot. Int J Pharm 1992;86:159-66.
Aburahma MH, Badr eldin SM. Compritol 888 ATO: a multifunctional lipid excipient in drug delivery systems and nanopharmaceuticals. Expert Opin Drug Delivery 2015;11 Suppl 12:1865-83.
Jannin V, Rodier JD, Musakhanian J. Polyoxylglycerides and glycerides: effects of manufacturing parameters on API stability, excipient functionality and processing. Int J Pharm 2014;466(1, Suppl 2):109-21.
Pople P, Singh KK. Glyceryl behenate. In: Rowe RC, Sheskey PJ, Owen SC. editors. Handbook of pharmaceutical excipients. American Pharma Assoc 2009;6:286-8.
Small DM. Lateral chain packing in lipids and membranes. J lipid Res 1984;25:1490-500.
Freitas C, Muller RH. Correlation between long-term stability of solid lipid nanoparticles (SLN) and crystallinity of the lipid phase. Eur J Pharm Biopharm 1999;47:125-32.
Souto SB, Mehnert W, Muller RH. Polymorphic behavior of compritol 888 ATO as a bulk lipid and as SLN and NLC. J Microbiol 2006;234:417-33.
Negi LM, Jaggi M, Talegaonkar S. Development of protocol for screening the formulation components and the assessment of common quality problems of nanostructured lipid carriers. Int J Pharm 2014;461:403-10.
Bose S, Du Y, Takhistov P. Formulation optimization and topical delivery of quercetin from solid lipid-based nanosystems. Int J Pharm 2013;441:56-66.
Rosenblatt KM, Bunjes H. Poly (vinyl alcohol) as emulsifier stabilizes solid triglyceride drug carrier nanoparticles in the alpha-modification. Mol Pharm 2008;6:105-20.
Maniruzzaman M, Slipper IJ, Vithani K, Douroumis D. Sustained release solid lipid matrices processed by hot-melt extrusion (HME). Colloids Surf B 2013;110:403-10.
Jannin V, Cuppok Y. Hot-melt coating with lipid excipients. Int J Pharm 2013;457:480-7.
European Pharmacopoeia. 6th edition. Council of Europe: Strasbourg; 2007.
United States Pharmacopeia 32 and National Formulary 27. United States Pharmacopeial Convention: Rockville, MD; 2009.
Food Chemicals Codex. edited by Institute of Medicine (U. S.). Committee on food chemicals codex. National Academies Press; 2003.
Bunjes H, Westesen K, Koch MHJ. Crystallization tendencies and polymorphic transitions in triglyceride nanoparticles. Int J Pharm 1996;129:159-73.
Jenning V, Thunemann AF, Gohla SH. Characterization of a novel solid lipid nanoparticle carrier system based on binary mixtures of liquid and solid lipids. Int J Pharm 2000;199:167-77.
Vivek K, Reddy H, Murthy RS. Investigations of the effect of the lipid matrix on drug entrapment, in vitro release, and physical stability of olanzapine-loaded solid lipid nanoparticles. AAPS PharmSciTech 2007;8:83.
Passerini N, Albertini B. Solid lipid microparticles produced by spray congealing: influence of the atomizer on microparticle characteristics and mathematical modeling of the drug release. J Pharm Sci 2010;99:916-31.
Kalasz H, Antal I. Drug excipients. Curr Med Chem 2006;13:2535-63.
Brossard C, Ratsimbazafy V, Des Ylouses DL. Modeling of theophylline compound release from hard gelatin capsules containing gelucire matrix granules. Drug Dev Ind Pharm 1991;17:1267-77.
Volkhard Jenning SHG. Encapsulation of retinoids in solid lipid nanoparticles (SLN). J Microbiol 2001;18:149-58.
Achanta AS, Adusumilli PS, James KW, Rhodes CT. Hot-melt coating: water sorption behavior of excipient films. Drug Dev Ind Pharm 2001;27:241-50.
Negi LM, Jaggi M, Talegaonkar S. Development of protocol for screening the formulation components and the assessment of common quality problems of nanostructured lipid carriers. Int J Pharm 2014;461:403-10.
Rosenblatt KM, Bunjes H. Poly (vinyl alcohol) as emulsifier stabilizes solid triglyceride drug carrier nanoparticles in the alpha-modification. Mol Pharm 2008;6:105-20.
Achanta AS, Adusumilli PS, James KW, Rhodes CT. Thermodynamic analysis of water interaction with excipient films. Drug Dev Ind Pharm 2001;27:227-40.
Hariharan M, Wowchuk C, Nkansah P, Gupta VK. Effect of formulation composition on the properties of controlled-release tablets prepared by roller compaction. Drug Dev Ind Pharm 2004;30:565-72.
Obaidat AA, Obaidat RM. Controlled release of tramadol hydrochloride from matrices prepared using glyceryl behenate. Eur J Pharm Biopharm 2001;52:231-5.
Jannin V, Berard V, Diaye NA, Andres C, Pourcelot Y. Comparative study of the lubricant performance of compritol 888 ATO either used by blending or by hot melt coating. Int J Pharm 2003;262:39-45.
Muller RH, Mader K, Gohla S. Solid lipid nanoparticles (SLN) for controlled drug delivery a review of state of the art. Eur J Pharm Biopharm 2000;50:161-77.
Gohla SH, Dingler A. Scaling up the feasibility of the production of solid lipid nanoparticles (SLN). Pharmazie 2001;56:61-3.
Manjunath K, Reddy JS, Venkateswarlu V. Solid lipid nanoparticles as drug delivery systems. Methods Find Exp Clin Pharmacol 2005;27:127-44.
Abdelbary G, Fahmy RH. Diazepam-loaded solid lipid nanoparticles: design and characterization. AAPS PharmSciTech 2009;10:211-9.
Gokce EH, Sandri G, Bonferoni MC. Cyclosporine loaded SLNs: evaluation of cellular uptake and corneal cytotoxicity. Int J Pharm 2008;364:76-86.
Report by Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, Mumbai. Narsee Monjee Institute of Management Studies, Mumbai; 2006.
Bodmeier RA, Swarbrick J, Boylan JC. Eds. Encyclopedia of pharmaceutical technology. 2nd ed. Vol. III. New York Marcel Dekkerlnc 1998;3 Suppl 2:2988-3000.
Hamdani J, Moes AJ, Amighi K. Physical and thermal characterization of precirol and compritol as lipophilic glycerides used for the preparation of controlled release matrix pellets. Int J Pharm 2003;260:47–57.
Zang YE, Schwartz JB. Melt granulation and heat treatment for wax matrix-controlled drug release. Drug Dev Ind Pharm 2003;29:131-8.
Zangenberg NH, Mullertz A, Kristensen HG, Hovgaard L. A dynamic in vitro lipolysis model. II. Evaluation of the model. Eur J Pharm Sci 2001;14:237-44.
PubChem. Available from: https://pubchem.ncbi.nlm.nih.gov. [Last accessed on 05 Apr 2019].
http: //www.americanpharmaceuticalreview.com. [Last accessed on 05 Apr 2019].
http://www.ferromet.com.arindex. [Last accessed on 05 Apr 2019].
Report by Shanghai Thanch Pharmaceuticals Technology Co., Ltd; 2011.
Martins A. Applying nanotechnology to human health: a revolution in biomedical sciences. J Biomed Nanotech 2009;5 Suppl 1:76.
https://www.trc-canada.com/structure-search/). [Last accessed on 05 Apr 2019].
Lide, David R. CRC Handbook of Chemistry and Physics. CRC Press; 2009.
Van Langevelde A, Peschar R, Schenk H. Structure of β-Trimyristin and β-tristearin from high-resolution X-ray powder diffraction data. Acta Crystallogr Sect B 2001;57 Suppl 3:372.
https://www.Cremercare.De. [Last accessed on 05 Apr 2019]
Bindu NHS, Kumar SR. In vitro assimilation of trimyristin in the seeds of myristica fragrans and in the polyherbal ayurvedic formulation by UFLC method. Asian J Pharm Clin Res 2013;6 Suppl 4:140-5.
Report by Institute of R and D, G. F. S. U. Gandhinagar, GUJARAT; 2011-2012.
Published
How to Cite
Issue
Section
