Microencapsulation of DEET in Solid Lipid Microparticles: production, characterization and safety evaluation

SANTOS, PAULA A.; SILVA, MÁRCIO R.M. DA; TAVARES, MELANIE; RICCI-JUNIOR, EDUARDO

doi:10.1590/0001-3765202220211166

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HEALTH SCIENCES • An. Acad. Bras. Ciênc. 94 (suppl 3) • 2022 • https://doi.org/10.1590/0001-3765202220211166 copy

Microencapsulation of DEET in Solid Lipid Microparticles: production, characterization and safety evaluation

Authorship SCIMAGO INSTITUTIONS RANKINGS

Abstract

DEET is considered the gold standard for insect repellent products. However, it behaves as a strong skin permeant. DEET was encapsulated in Solid Lipid Microparticles (SLM) and characterized in terms of morphology, particle size, cytotoxicity and ex vivo permeation. The particles exhibited micrometric size with a spherical shape. In addition, we developed and validated an analytical method for DEET quantification by high performance liquid chromatography (HPLC), which was selective, linear, precise, accurate and robust. The toxicity test in cell culture of keratinocytes, fibroblasts and macrophages showed that the formulation did not present cytotoxicity. The SLM were able to decrease the skin permeation of DEET in relation to the free active in ethanol with gain in the safe. Microparticles were able to increase the skin retention of DEET, which can contribute to extend the time of repellent action. The results showed that Solid Lipid Microparticles are safe and promising topical formulation to insect bite prevention.

Key words
DEET; Solid Lipid Microparticles; Ex vivo permeation; Cytotoxicity

Formulation	Estearic acid	DEET	Polysorbate 80	Methylparaben	Water (EQF)
1	10%	10%	5%	0.1%	20 mL

Formulation	DEET	pH	Span	Size ( µm)
1	10%	5.72±0121	5.04±0.38	62.53±1.75

Solution	Rating criteria
Calibration ICRS	DPR (%) of the replicate areas must be ≤ 1.0%
Resolution (R)	Minimum 1.5
Theoretical dishes (N)	Minimum 2000
Tail factor	Maximum 2.0

Parameters	DEET (Content / RSD)	Acceptance criteria
Selectivity	No interference	No interference
Linearity	0.998	r > 0.990
Precision^a	105.63 ± 0.66 %	< 5%
Precision^b	106.09 ± 0.38 %	< 5%
Accuracy (80%)^c	95.75 ± 0.43 %	< 5%
Accuracy (100%)^d	97.26 ± 0.65 %	< 5%
Accuracy (120%)^e	104.01 ± 0.24 %	< 5%
QL (µg/mL)	20	-
DL (µg/mL)	9.5	-

Parameters	Tail factor	Retention time (min)	Area	Content (%)	RSD
Flow (mL)
0.8	1.423	14.909	3386206	102	0.07
1.0*	1.386	11.861	2621918	102	0.45
1.2	1.430	9.855	2221871	102	0.10
Temperature (°C)
23	1.285	11.807	2701555	96	0.16
25*	1.462	11.545	2897039	106	0.10
27	1.349	11.216	2706143	92	0.05
Filter (µm)
0.22	1.124	11.906	3204803	104	0.11
Without filtering*	1.118	11.893	2857437	98	0.09
0.45	1.124	11.906	2860110	98	0.63
Column
ACE®*	1.628	11.761	2170480	100	0.52
Merck®	1.170	16.259	2830736	97	0.13
Mobile phase
MP 1	1.328	7.605	3123513	106	0.46
MP*	1.158	10.903	3076827	105	0.35
MP 2	1.153	19.293	3362162	105	0.46
Stability ICRS
Recent preparation	1.092	11.157	2959298	98	0.11
After 24 h	1.141	11.779	2977677	104	0.21
Sample stability
Recent preparation	1.076	11.173	3030089	105	0.28
After 24 h	1.123	11.694	3027842	104	0.27

Degradation condition	Content (%)	Peak purity
	API
Acid	108	0.99999
Basic	108	1.0000
Oxidizing	105	0.99999
Metal Ion	108	0.99999
Temperature	98.18	1.0000
Photostability	104.47	0.99999
	Sample
Acid	98	0.99999
Basic	99	0.99999
Oxidizing	100	0.99999
Metal Ion	95	0.99999
Temperature	147.90	1.0000
Photostability	128.32	1.0000

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[1] Correspondence to: Eduardo Ricci-Junior E-mail: ricci@pharma.ufrj.br