Academic Journal
Using mixtures of linoleic acid, a long-chain polyunsaturated fatty acid, and its monoglyceride in lipid-based formulations to increase drug loading and enhance aqueous microemulsification.
| Τίτλος: | Using mixtures of linoleic acid, a long-chain polyunsaturated fatty acid, and its monoglyceride in lipid-based formulations to increase drug loading and enhance aqueous microemulsification. |
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| Συγγραφείς: | Kandagatla HP; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, NY 11439, USA., Chowdhury N; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, NY 11439, USA., Verbić TŽ; University of Belgrade - Faculty of Chemistry, Studentski trg 12-16, 11000 Belgrade, the Republic of Serbia., Avdeef A; in-ADME Research, Walnut Creek, CA 94595, USA., Savoy A; School of Life Sciences, University of Applied Sciences and Arts Northwestern Switzerland, CH 4132 Muttenz, Switzerland., Kuentz M; School of Life Sciences, University of Applied Sciences and Arts Northwestern Switzerland, CH 4132 Muttenz, Switzerland., Serajuddin ATM; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, NY 11439, USA. Electronic address: serajuda@stjohns.edu. |
| Πηγή: | International journal of pharmaceutics [Int J Pharm] 2026 Oct 05; Vol. 703, pp. 127369. Date of Electronic Publication: 2026 Sep 01. |
| Τύπος έκδοσης: | Journal Article |
| Γλώσσα: | English |
| Στοιχεία περιοδικού: | Publisher: Elsevier/North-Holland Biomedical Press Country of Publication: Netherlands NLM ID: 7804127 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1873-3476 (Electronic) Linking ISSN: 03785173 NLM ISO Abbreviation: Int J Pharm Subsets: MEDLINE |
| Imprint Name(s): | Original Publication: Amsterdam, Elsevier/North-Holland Biomedical Press. |
| Ιατρικοί όροι (MeSH): | Monoglycerides*/chemistry , Linoleic Acid*/chemistry, Emulsions/chemistry ; Water/chemistry ; Lipids/chemistry ; Chemistry, Pharmaceutical/methods ; Solubility ; Drug Delivery Systems ; Drug Compounding ; Glycerides |
| Περίληψη: | Although lipid-based formulations (LBFs) of self-emulsifying drug delivery systems (SEDDS) have been used for poorly water-soluble drugs, they have many limitations, the first being the low solubility of drugs in lipids, which limits drug loading in formulations, and the second being inadequate dispersion of formulations in the aqueous fluids of the human gastrointestinal tract (GIT). Large amounts of organic cosolvents and surfactants, up to 90% of the formulation, have been used to overcome these limitations. We previously demonstrated that the situation could be improved by using lipid digestion products (LDP), which consist of a 2:1 molar ratio of long-chain fatty acids and monoglycerides, rather than lipids (triglycerides) themselves. The drug solubility and, therefore, drug loading in the formulations increased greatly in the presence of a long-chain fatty acid in the LDP. However, only one acid, oleic acid (OA), and its monoglyceride were used in those studies. To demonstrate the versatility of the approach, a different LDP, another acid, linoleic acid (LA), and its monoglyceride, glyceryl monolinoleate (GML), were used at a 2:1 molar ratio in the present study, with clofazimine (CFZ) as the model drug. Although both OA and LA are C-18 fatty acids, the latter has two double bonds instead of one, which affects its physicochemical properties, such as pK (Copyright © 2026 Elsevier B.V. All rights reserved.) |
| Competing Interests: | Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. |
| Contributed Indexing: | Keywords: Dispersion test; Drug solubility; Linoleic acid; Lipid digestion products; Lipid-based formulation; Long-chain fatty acid; Maisine®; Microemulsion; Molecular dynamics simulation; SEDDS |
| Substance Nomenclature: | 0 (Monoglycerides) 9KJL21T0QJ (Linoleic Acid) 0 (Emulsions) 059QF0KO0R (Water) 0 (Lipids) MGG581HK1Y (monolinolein) 0 (Glycerides) |
| Entry Date(s): | Date Created: 20260901 Date Completed: 20260919 Latest Revision: 20260919 |
| Update Code: | 20260920 |
| DOI: | 10.1016/j.ijpharm.2026.127369 |
| PMID: | 42679973 |
| Βάση Δεδομένων: | MEDLINE |
| ISSN: | 1873-3476 |
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| DOI: | 10.1016/j.ijpharm.2026.127369 |