Abstract
Purpose: To formulate self-nanoemulsifying drug delivery systems (SNEDDS) based on melon oil and its admixture with a homolipid from Bos indicus (cow fat) for the delivery of indomethacin, a hydrophobic anti-inflammatory agent. Method: Melon oil and cow fat were extracted by standard methods and used in the formulation of SNEDDS based on either melon oil alone, or its admixture with cow fat by utilizing varying ratios of oil(s), surfactants and co-surfactants, with or without carbosil, a glidant. The formulations were encapsulated in hard gelatin capsules and then evaluated using relevant parameters including isotropicity tests, dilution stability, precipitation propensity, emulsification time, absolute drug content, in vitro drug release, and anti-inflammatory activity in an animal model. Results: Stable and negatively charged colloidal dispersions (zeta potential: -10.4 to -13.4 mV) in the nano size range (195 - 210 nm) were formed. Formulation of indomethacin as SNEDDS not only preserved the activity of the drug, but also guaranteed anti-inflammatory activity comparable to that of indomethacin injection. The inhibition produced by the drug-loaded SNEDDS and the positive control were identical for much of the 5 h test period, indicating a high degree of bioavailability of the administered SNEDDS formulation. Conclusion: A 1:1 ratio of melon oil and cow fat could be used in the formulation and delivery of indomethacin-loaded SNEDDS with satisfactory properties and acceptable product performance. The anti-inflammatory activity of indomethacin was preserved in the formulation.
Highlights
Self-emulsifying drug delivery system (SEDDS) is a strategy that has drawn wide research interest, basically due to its distinct capacity to solubilise and improve the bioavailability of poorly water-soluble drugs. This it does by ensuring aqueous solubility of the lipophilic drug
The objective of this study was to investigate the suitability of melon oil, or its admixture with a homolipid from Bos indicus, for use as the oily component for indomethacin-loaded self-nanoemulsifying drug delivery systems (SNEDDS), using standard non-toxic surfactants
All batches of the formulated SNEDDS retained their isotropicity after a ten-fold dilution
Summary
Self-emulsifying drug delivery system (SEDDS) is a strategy that has drawn wide research interest, basically due to its distinct capacity to solubilise and improve the bioavailability of poorly water-soluble drugs. This it does by ensuring aqueous solubility of the lipophilic drug. Aqueous solubility is an important molecular property required for successful drug development. This is because it strongly determines drug accessibility to biological membranes [1]. This, amongst others, is the major disadvantage self-emulsifying formulations (SEOFs) seek to circumvent [3]
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