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BMC Complementary Medicine and Therapies
Published in: BMC Complementary Medicine and Therapies 1/2023

Open Access 01-12-2023 | Ibuprofen | Research

Enhanced anti-inflammatory and ulcerogenicity of Ibuprofen microsphere formulations using Irvingia wombolu fat (IRW) and moringa oil (MO) as co-lipids

Authors: Thaddeus H. Gugu, Geraldine C. Agu, Emmanuel M. Uronnachi, Salome A. Chime

Published in: BMC Complementary Medicine and Therapies | Issue 1/2023

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Abstract

Ibuprofen is a member of the propionic acid class of nonsteroidal anti-inflammatory drugs (NSAIDs) with anti-inflammatory, analgesic, and antipyretic activities used to relieve a variety of pains. The objective of this study was to formulate, characterize and evaluate the in vitro and in vivo properties of ibuprofen formulated as solid lipid microspheres (SLMs) for enhanced delivery. The mixtures of Irvingia wombolu fat (IRW) and moringa oil (MO) each with Phospholipon® 90G (PL90G) at the ratio of 2:1 w/w were prepared by fusion, characterized and used to prepare SLMs. The SLMS were thereafter evaluated using the following parameters: particle size and morphology, stability, and encapsulation efficiency EE (%). In vitro release was carried out in phosphate buffer (pH 7.4). The ibuprofen based SLMs were also evaluated for anti-inflammatory and anti-ulcer effects using animal models. The pH showed significant increase after two months of formulation with a maximum value of 6.4 while the EE obtained were 95.6, 89.4 and 61.6% for SLMs formulated with lipid matrix of Phospholipon® 90G (1% and 2%), and MO (1%) respectively. The in vitro release showed maximum release of 87.8 and 98.97% of the two different lipid-based formulations while anti-inflammatory effect was up to 89.90% after 5 h of inducing inflammation. The SLMs did not show any lesion thus conferring gastroprotection on the formulations. The SLMs exhibited good anti-inflammatory property with gastroprotective action.
Literature
1.
Ngo VTH and Bajaj T, Ibuprofen, in StatPearls. 2022, StatPearls Publishing Copyright © 2022, StatPearls Publishing LLC.: Treasure Island (FL).
2.
Brunton L, Chabner B, Knollman B. Goodman and Gilman’s The Pharmacological basis of therapeutics. 12th ed. New York: McGraw-Hill; 2010.
3.
Rivers-Auty J, Mather AE, Peters R, Lawrence CB, Brough D. Anti-inflammatories in Alzheimer’s disease-potential therapy or spurious correlate? Brain Commun. 2020;2(2):fcaa109.CrossRefPubMedPubMedCentral
4.
Jørgensen B, Friis GJ, Gottrup F. Pain and quality of life for patients with venous leg ulcers: proof of concept of the efficacy of Biatain-Ibu, a new pain reducing wound dressing. Wound Repair Regen. 2006;14(3):233–9.CrossRefPubMed
5.
Ofek L, Goder D, Zilberman M. Formulation-Properties of Novel Ibuprofen-Loaded Soy Protein Wound Dressings. Recent Progress in Materials. 2019;01(04):004.
6.
Ghlichloo I and Gerriets V, Nonsteroidal Anti-inflammatory Drugs (NSAIDs), in StatPearls. 2022, StatPearls Publishing
7.
Banerjee S, Pillai J. Solid lipid matrix mediated nanoarchitectonics for improved oral bioavailability of drugs. Expert Opin Drug Metab Toxicol. 2019;15(6):499–515.CrossRefPubMed
8.
Nanjwade BK, Patel DJ, Udhani RA, Manvi FV. Functions of lipids for enhancement of oral bioavailability of poorly water-soluble drugs. Sci Pharm. 2011;79(4):705–27.CrossRefPubMedPubMedCentral
9.
Kumar A, Lahiri SS, Singh H. Development of PEGDMA: MAA based hydrogel microparticles for oral insulin delivery. Int J Pharm. 2006;323(1–2):117–24.CrossRefPubMed
10.
Momoh M, Kenechukwu F, Gwarzo M, Builders P. Formulation and Evaluation of Ibuprofen Loaded Lipospheres for Effective Oral Drug Delivery. Dhaka University Journal of Pharmaceutical Sciences. 2015;14(1):17–27.CrossRef
11.
Matsinkou R, Ngondi J, Kuate D, Mbofung C, and Oben J, Antioxidant and anti-hyperglycemic potential of pulp extracts of Irvingia wombolu fruits. Biology and Medicine, 2012. 4: p. 10+.
12.
Onyishi IV, Chime SA, Attama AA. Evaluation of excipient potentials of Irvingia wombolu fats and Moringa oil in rifampicin-loaded lipospheres: in vitro-in vivo characterisation. Journal of Drug Delivery Science and Technology. 2014;24(4):404–12.CrossRef
13.
Alam D, Singh MP, and Singh A, Wound healing potential of some medicinal plants. International Journal of Pharmaceutical Sciences Review and Research, 2011. 9.
14.
Eugenia Nonye O, Okeke CC. Determination of antioxidant of Moringa oleifera seed oil and its use in the production of a body cream. Asian J Plant Sci Res. 2013;3:1–4.
15.
Hu FQ, Yuan H, Zhang HH, Fang M. Preparation of solid lipid nanoparticles with clobetasol propionate by a novel solvent diffusion method in aqueous system and physicochemical characterization. Int J Pharm. 2002;239(1–2):121–8.CrossRefPubMed
16.
Lippacher A, Müller RH, Mäder K. Preparation of semisolid drug carriers for topical application based on solid lipid nanoparticles. Int J Pharm. 2001;214(1–2):9–12.CrossRefPubMed
17.
Jaspart S, Bertholet P, Piel G, Dogné JM, Delattre L, Evrard B. Solid lipid microparticles as a sustained release system for pulmonary drug delivery. Eur J Pharm Biopharm. 2007;65(1):47–56.CrossRefPubMed
18.
Pardeshi C, Rajput P, Belgamwar V, Tekade A, Patil G, Chaudhary K, Sonje A. Solid lipid based nanocarriers: an overview. Acta Pharm. 2012;62(4):433–72.CrossRefPubMed
19.
Ahmed OAA, Fahmy UA, Bakhaidar R, El-Moselhy MA, Alfaleh MA, Ahmed AF, Hammad ASA, Aldawsari H, Alhakamy NA. Pumpkin Oil-Based Nanostructured Lipid Carrier System for Antiulcer Effect in NSAID-Induced Gastric Ulcer Model in Rats. Int J Nanomedicine. 2020;15:2529–39.CrossRefPubMedPubMedCentral
20.
Gigliobianco MR, Casadidio C, Censi R, Di Martino P. Nanocrystals of Poorly Soluble Drugs: Drug Bioavailability and Physicochemical Stability. 2018;10(3):134.
21.
Misra SK and Pathak K, Chapter 10 - Drug nanocrystals as drug delivery systems, in Industrial Applications of Nanocrystals, S. Mallakpour and C.M. Hussain, Editors. 2022, Elsevier. p. 153–178.
22.
Bhalani DV, Nutan B, Kumar A, Singh Chandel AK. Bioavailability Enhancement Techniques for Poorly Aqueous Soluble Drugs and Therapeutics. 2022;10(9):2055.
23.
Chime SA, Attama AA, Onunkwo GJJoDDS, and Technology, Sustained release indomethacin-loaded solid lipid microparticles based on solidified reverse micellar solution (SRMS): in vitro and in vivo evaluation. 2012. 22: p. 485–492.
24.
Umeyor EC, Kenechukwu FC, Ogbonna JD, Chime SA, Attama A. Preparation of novel solid lipid microparticles loaded with gentamicin and its evaluation in vitro and in vivo. J Microencapsul. 2012;29(3):296–307.CrossRefPubMed
25.
Attama AA, Okafor CE, Builders PF, Okorie O. Formulation and in vitro evaluation of a PEGylated microscopic lipospheres delivery system for ceftriaxone sodium. Drug Deliv. 2009;16(8):448–57.CrossRefPubMed
26.
Abobakr FE, Fayez SM, Elwazzan VS, Sakran W. Effect of Different Nail Penetration Enhancers in Solid Lipid Nanoparticles Containing Terbinafine Hydrochloride for Treatment of Onychomycosis. AAPS PharmSciTech. 2021;22(1):33.CrossRefPubMed
27.
Lalan BK, Hiray RS, and Ghongane BB, Evaluation of Analgesic and Anti-Inflammatory Activity of Extract of Holoptelea Integrifolia and Argyreia Speciosa in Animal Models. J Clin Diagn Res, 2015. 9(7): p. Ff01–4.
28.
Anosike CA, Obidoa O, Ezeanyika LUS, and Nwuba MMJAJoBR, Anti-inflammatory and anti-ulcerogenic activity of the ethanol extract of ginger (Zingiber officinale). 2009. 3: p. 379–384.
29.
Karim N, Khan I, Khan W, Khan I, Khan A, Halim SA, Khan H, Hussain J, and Al-Harrasi A, Anti-nociceptive and Anti-inflammatory Activities of Asparacosin A Involve Selective Cyclooxygenase 2 and Inflammatory Cytokines Inhibition: An in-vitro, in-vivo, and in-silico Approach. 2019. 10.
30.
Gugu TH, Chime SA, Attama AA. Solid lipid microparticles: An approach for improving oral bioavailability of aspirin. Asian J Pharm Sci. 2015;10(5):425–32.CrossRef
31.
Chung MC, dos Santos JL, Oliveira EV, Blau L, Menegon RF, Peccinini RG. Synthesis, ex vivo and in vitro hydrolysis study of an indoline derivative designed as an anti-inflammatory with reduced gastric ulceration properties. Molecules. 2009;14(9):3187–97.CrossRefPubMedPubMedCentral
32.
Fahy E, Subramaniam S, Murphy RC, Nishijima M, Raetz CR, Shimizu T, Spener F, van Meer G, Wakelam MJ, and Dennis EA, Update of the LIPID MAPS comprehensive classification system for lipids. J Lipid Res, 2009. 50 Suppl(Suppl): p. S9–14.
33.
Subramaniam S, Fahy E, Gupta S, Sud M, Byrnes RW, Cotter D, Dinasarapu AR, Maurya MR. Bioinformatics and systems biology of the lipidome. Chem Rev. 2011;111(10):6452–90.CrossRefPubMedPubMedCentral
34.
Garud A, Singh D, Garud N. Solid Lipid Nanoparticles (SLN): Method, Characterization and Applications. International Current Pharmaceutical Journal. 2012;1(11):384–93.CrossRef
35.
Ong SG, Ming LC, Lee KS, and Yuen KH, Influence of the Encapsulation Efficiency and Size of Liposome on the Oral Bioavailability of Griseofulvin-Loaded Liposomes. Pharmaceutics, 2016. 8(3).
36.
Audu MM, Achile PA, and Amaechi AAJPJoZ, Phospholipon 90G based SLMs loaded with ibuprofen: an oral antiinflammatory and gastrointestinal sparing evaluation in rats. 2012. 44: p. 1657–1664.
37.
Puglia C, Blasi P, Rizza L, Schoubben A, Bonina F, Rossi C, Ricci M. Lipid nanoparticles for prolonged topical delivery: an in vitro and in vivo investigation. Int J Pharm. 2008;357(1–2):295–304.CrossRefPubMed
38.
Anthony AA, Mumuni AM, and Philip FB, Lipid Nanoparticulate Drug Delivery Systems: A Revolution in Dosage Form Design and Development, in Recent Advances in Novel Drug Carrier Systems, S. Ali Demir, Editor. 2012, IntechOpen: Rijeka. p. Ch. 5.
39.
Wissing SA, Kayser O, Müller RH. Solid lipid nanoparticles for parenteral drug delivery. Adv Drug Deliv Rev. 2004;56(9):1257–72.CrossRefPubMed
40.
Abdul W, Pre-formulation investigation and in vitro evaluation of directly compressed ibuprofen-ethocel oral controlled release matrix tablets: A kinetic approach. African Journal of Pharmacy and Pharmacology, 2011. 5(19).
41.
Popova AV, Hincha DK. Thermotropic phase behavior and headgroup interactions of the nonbilayer lipids phosphatidylethanolamine and monogalactosyldiacylglycerol in the dry state. BMC Biophys. 2011;4(1):11.CrossRefPubMedPubMedCentral
42.
43.
Scherphof GL, Velinova M, Kamps J, Donga J, van der Want H, Kuipers F, Havekes L, Daemen T. Modulation of pharmacokinetic behavior of liposomes. Adv Drug Deliv Rev. 1997;24(2):179–91.CrossRef
44.
Chime SA, Attama AA, Builders PF, Onunkwo GC. Sustained-release diclofenac potassium-loaded solid lipid microparticle based on solidified reverse micellar solution: in vitro and in vivo evaluation. J Microencapsul. 2013;30(4):335–45.CrossRefPubMed
45.
AshokKumar J, Ramkanth, Prabu L, and Gopal. Enhancement of Saturation Solubility and In Vitro Dissolution of Carvedilol Nanoparticles by High Pressure Homogenization Technique. 2015.
46.
Bolourtchian N, Karimi K, Aboofazeli R. Preparation and characterization of ibuprofen microspheres. J Microencapsul. 2005;22(5):529–38.CrossRefPubMed
47.
Mady O. Ibuprofen encapsulation by eudragit RS100 as microspheres: preparation and drug release. MOJ Bioequiv Availab. 2017;4(1):193–9.
48.
Al-Thamarani S, Gardouh A. Enhanced oral bioavailability and gastroprotective effect of ibuprofen through mixed polymer–lipid nanoparticles. Ther Deliv. 2021;12(5):363–74.CrossRefPubMed
49.
Almeida H, Amaral MH, Lobão P. Comparative study of sustained-release lipid microparticles and solid dispersions containing ibuprofen. Braz J Pharm Sci. 2012;48(3):529–36.CrossRef
50.
51.
Rea IM, Gibson DS, McGilligan V, McNerlan SE, Alexander HD, Ross OA. Age and Age-Related Diseases: Role of Inflammation Triggers and Cytokines. Front Immunol. 2018;9:586.CrossRefPubMedPubMedCentral
52.
Shinde AJ, Patil NC. DESIGN AND DEVELOPMENT OF NANOSTRUCTURED LIPID CARRIER CONTAINING TRIAMCINOLONE ACETONIDE. Int J Pharm Pharm Sci. 2019;11(12):26–35.
Metadata
Title
Enhanced anti-inflammatory and ulcerogenicity of Ibuprofen microsphere formulations using Irvingia wombolu fat (IRW) and moringa oil (MO) as co-lipids
Authors
Thaddeus H. Gugu
Geraldine C. Agu
Emmanuel M. Uronnachi
Salome A. Chime
Publication date
01-12-2023
Publisher
BioMed Central
Keyword
Ibuprofen
Published in
BMC Complementary Medicine and Therapies / Issue 1/2023
Electronic ISSN: 2662-7671
DOI
https://doi.org/10.1186/s12906-023-04036-2

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