Design, preparation and <i>in vitro</i> characterizations of fluconazole loaded nanostructured lipid carriers

Fernandes, Amanda Velinna; Pydi, Chinna Raja; Verma, Ruchi; Jose, Jobin; Kumar, Lalit

doi:10.1590/s2175-97902019000318069

Amanda Velinna Fernandes

Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Udupi, Karnataka, India,

Chinna Raja Pydi

Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Udupi, Karnataka, India,

Ruchi Verma

Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Udupi, Karnataka, India,

http://orcid.org/0000-0002-1279-7243

Jobin Jose

Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, NITTE Deemed to be University, Paneer, Deralakatte, Mangalore, India

Lalit Kumar ^**Correspondence: L. Kumar. Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal 576 104, Karnataka, India. Phone: +91 98801 20144. E-Mail: lk.kundlas@gmail.com

Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Udupi, Karnataka, India,

*Correspondence: L. Kumar. Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal 576 104, Karnataka, India. Phone: +91 98801 20144. E-Mail: lk.kundlas@gmail.com

DISCLOSURE

The authors declared that there is no conflict of interest in this work.

Surfactant	Concentration	Amount of SA (mg)	Amount of castor oil (µL)	Particle size (nm)	PDI	Zeta potential (mV)
Poloxamer 188	2 %w/v	200	20	1813	0.414	-19.6
Tween 80	2 %v/v	200	20	817.9	0.560	-3.9
Tween 20	2 %v/v	200	20	1311	0.409	-23.7

Surfactant	Concentration (%v/v)	Amount of SA (mg)	Amount of castor oil (µL)	Particle size (nm)	PDI	Zeta potential (mV)
Tween 80	2	200	20	520.5	0.302	-21.5
Tween 20	2	200	20	362.4	0.216	-21.6
Tween 20	2	200	40	383.2	0.266	-25.9
Tween 20	2	300	40	169.1	0.481	-20.4

Variables	Levels
Variables	-1	+1
Amount of lipid (mg)	200	300
Surfactant concentration (%v/v)	2	3
Sonication amplitude (W)	21 ± 2	27 ± 2

Vibration mode	Frequency (cm^-1)
Vibration mode	FLZ	SA	PM
N-H Str	3111.18	----	3111.18
C-H Str	2958.80	----	2956.87
C-H Str	----	2927.94	----
C-H Str	----	2852.72	2852.72
O-H Str	----	2673.34	----
C=O Str	----	1707.00	1708.93
C=C Str	1595.13	----	1595.13
Triazole ring Str	1510.26	----	1510.26
C-OH Str	----	1411.89	1423.47
Triazole ring Str	1247.94	----	1247.94
C-F Str	1139.93	----	1138.00
C-OH Str	1016.86	1099.43	1011.86
O-H Str	966.34	941.26	966.34
b-CF	572.86	----	572.86

Vibration mode	Frequency (cm^-1)
Vibration mode	FLZ	SA	TW	CO	SFLZ	SCFLZ	SCTFLZ
O-H Str.	----	----	3481.98	----	----	----	3442.62
C-H Str	3105.00	----	----	----	3116.05	3118.05	3117.78
C-H Str	2956.31	----	----	----	2956.32	2955.99	----
C-H Str.	----	2914.20	2921.68	----	2914.81	2916.09	2918.13
C-H Str.	----	2847.17	2861.48	----	2847.54	2849.02	2852.11
-C-H- Str.	----	----	----	2924.61	----	2916.09	2918.13
-C=O Str.	----	----	1734.66	1742.80	----	1744.21	1740.24
C=O Str	----	1696.36	----	----	1698.97	1701.78	1703.78
C=C Str.	1616.77	----	----	----	1616.55	1616.59	1616.93
Triazole ring str.	1502.33	----	----	----	1514.48	1514.47	1513.84
C-F Str	1274.31	----	----	----	1270.68	1269.84	1270.98
Triazole ring Str.	1246.47	----	----	----	1250.27	1250.82	1250.07
C-OH Str	1016.86	----	----	----	1011.61	1010.57	1011.19

Formulation code	Variables			Responses
Formulation code	Amount of lipid (mg)	Surfactant concentration (% v/v)	Sonication amplitude (W)	Particle size (nm)	PDI	Zeta potential (mV)
NLC 1	200	2	21 ± 2	391.10	0.181	-17.40
NLC 2	200	2	27 ± 2	342.10	0.209	-16.50
NLC 3	200	3	21 ± 2	386.50	0.413	-18.00
NLC 4	200	3	27 ± 2	355.40	0.203	-15.60
NLC 5	300	2	21 ± 2	418.00	0.197	-18.60
NLC 6	300	2	27 ± 2	259.50	0.284	-14.30
NLC 7	300	3	21 ± 2	393.10	0.165	-14.80
NLC 8	300	3	27 ± 2	400.40	0.475	-21.00

Factors	Particle size			PDI			Zeta potential
Factors	Coefficient estimate	F-value	p-value	Coefficient estimate	F-value	p-value	Coefficient estimate	F-value	p-value
Intercept	368.260	----	----	0.270	----	----	- 17.03	----	----
A	----	----	----	0.014	5.610	0.141	----	----	----
B	15.590	925.050	0.021	0.048	62.890	0.016	----	----	----
C	- 28.910	3182.610	0.011	0.027	19.610	0.047	----	----	----
AB	13.410	684.910	0.024	----	----	----	- 0.400	3.020	0.180
AC	- 8.890	300.730	0.037	0.072	142.230	0.007	- 0.650	7.980	0.066
BC	22.960	2007.480	0.014	----	----	----	- 1.130	23.920	0.016
ABC	18.490	1301.270	0.018	0.058	90.170	0.011	- 1.500	42.520	0.007
R²	0.999			0.994			0.963
Adj R²	0.999			0.978			0.913
Adeq precision	116.89			21.11			12.73

	Variables			Responses			Desirability
	A (mg)	B (%v/v)	C (W)	PS (nm)	PDI	ZP (mV)	Desirability
Software Suggested	252.56	2.01	26.98	300.00	0.247	-15.87	0.970
Actual Obtained	252.00	2.00	27.00	359.15 ± 9.83	0.236 ± 0.01	-19.25 ± 0.35
Residual values	----	----	----	-59.15	0.011	-3.38

[1] *Correspondence: L. Kumar. Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal 576 104, Karnataka, India. Phone: +91 98801 20144. E-Mail: lk.kundlas@gmail.com

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Design, preparation and in vitro characterizations of fluconazole loaded nanostructured lipid carriers