A review on lipid-based nanocarriers mimicking chylomicron and their potential in drug delivery and targeting infectious and cancerous diseases

Elnady, Rana E.; Amin, Maha M.; Zakaria, Mohamed Y.

doi:10.1186/s41120-023-00080-x

AAPS Open

Table 3 Therapeutic applications of EMLs in infectious diseases

From: A review on lipid-based nanocarriers mimicking chylomicron and their potential in drug delivery and targeting infectious and cancerous diseases

S. No	Drug	Indication	Components	Method	PS	EE%	Animal or cell line model	Purpose of study	Outcomes	Ref
1	Sparfloxacin	Ophthalmic anti-bacterial	CA, P90G	TFH	217 ± 3.78 nm	72.83 ± 2.56%	Male albino rabbits	Determination of the biological activity of EMLs–gel system compared with pure drug solution against microorganisms	• Sustained drug release, formulation with non-irritant and promising anti-bacterial action both in vitro and in vivo • The infection disappeared within (4–5 days)	Sawant et al. 2016)
1	Sparfloxacin	Ophthalmic anti-bacterial	CA, P90G	TFH	217 ± 3.78 nm	72.83 ± 2.56%	Organism (S. aureus)			Sawant et al. 2016)
2	Silybin	Hepatitis and cirrhosis	Trilaurin, Soybean PC (> 94%). Chol, tween80	TFH	364.1 ± 20 nm	> 80%	Male Wistar rats	Comparing pharmacokinetic parameters between silybin-EMLs and pure drug solution	• Improved bioavailability, sustained release profile, increased mean residence time by 2.5-folds • Targeting the drug to liver increasing its rate and extent	Zhou and Chen 2015)
3	Zidovudine	Hepatitis	Tristearin, trilaurin, soya PC, Chol, stearylamine	TFH	130 ± 18 to 142 ± 22 nm	57.8 ± 6.2% (Tristearin) and 59.7 ± 6.1% (Trilaurin)	Albino rats	Comparing organ distribution of zidovudine-EMLs and free drug	• Reduced toxicity with liver targeting and prolonged action	Vyas et al. 2006)
4	Amphotericin B (AMB)	Visceral leishmaniasis	Soya PC, stearylamine, Chol, tripalmitin	TFH	plain EMLs (0.529 ± 0.016 µm) and coated EMLs (0.646 ± 0.015 µm)	Plain EMLs (78.1 ± 2.29) and coated EMLs (77.5 ± 2.95) %	Albino rats	Comparing organ distribution of amphotericin B-EMLs and free drug	• AMB-loaded OPM-EMLs showed (62.76 ± 3.54) % higher parasitic inhibition than the AMB-EMLs (42.68 ± 2.36) % and free AmB (25.87 ± 3.87) % • Higher drug EMLs concentration in macrophage-rich organs than plain AMB	Pal et al. 2012)
5	Bifonazole	Anti-fungal for skin or mucosal mycoses	Lecithin, Tristearin, Chol, Stearylamine (Octadecyl amine)	TFH	390.394 nm	81.642%	-	Optimization of emulsomal formulation using Box-Behnken design	• The optimized formulation achieved higher EE%, ZP, and minimum PS	Malviya 2021)
6	Bisnapthalimidopr-opyl derivatives (BNIPDaoct and BNIPDanon)	Anti-leishmanial therapy	Tripalmitin ≥ 99%, DPPC, ∼ 99%, Chol	TFH	363.1 ± 51.7 nm	-	Macrophages infected with Leishmania infantum parasites	Comparing the IC50 of drugs-EMLs and free drugs	• Drug-EMLs demonstrated higher cytotoxic activity by two folds	Islek et al. 2022)
7	Morin hydrate (MH)	Anti-MERS-CoV	PC (lecithin), triolein, Brij52 (polyoxyethylene (2) cetyl ether), CA	TFH	177.3 ± 18.9 nm	79.1 ± 2.2%	Vero E6 cells	Determination of the anti-viral activity against MERS-CoV	• MH-EMLs increased permeation by four times more than free MH • Suppressed MERS-CoV-induced histopathological alterations in lung tissue • Reduce the levels of oxidative and inflammatory biomarkers	Zakaria et al. 2022a)
7	Morin hydrate (MH)	Anti-MERS-CoV		TFH	177.3 ± 18.9 nm	79.1 ± 2.2%	Respiratory tract of the infected mice	Determination of the anti-viral activity against MERS-CoV		Zakaria et al. 2022a)
8	Resveratrol (RSV)	Anti-MERS-CoV	CA or tristearin, (DSPE-mPEG 2000), Chol	TFH	172.1 ± 19.5 nm	75.8 ± 3.7%	Vero E6 cells	Determination of the anti-viral activity against MERS-CoV	• Suppress the inflammatory response and oxidative stress resulting from MERS-CoV 26 times more than RSV dispersion	Zakaria et al. 2022b)
8	Resveratrol (RSV)	Anti-MERS-CoV	CA or tristearin, (DSPE-mPEG 2000), Chol	TFH	172.1 ± 19.5 nm	75.8 ± 3.7%	Respiratory tract of the infected mice	Determination of the anti-viral activity against MERS-CoV		Zakaria et al. 2022b)

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