Development and characterization of lecithin stabilized glibenclamide nanocrystals for enhanced solubility and drug delivery

Figures & data

Table 1. DL and PY of LNCs.

Batch	Drug:polymer composition	DL (%)	PY (%)
F1	1:1	50.08 ± 1.13	82.83 ± 3.01
F2	1:2	49.00 ± 0.69	73.89 ± 4.00
F3	1:4	40.66 ± 1.53	63.10 ± 2.76
F4	1:8	34.18 ± 0.21	61.63 ± 3.17
F5	2:1	51.18 ± 1.08	71.20 ± 3.93

Each formulation contains Tween 80 (3% w/v) as surfactant and LEC (2% w/v) complexing agent. ± Indicates SD (n = 3).

Figure 1. OC plot of LNCs.

Table 2. SL data of GLB and LNCs.

Batch	Drug:polymer composition (% w/w)	SL (mg/ml)	Percentage solubility (mg/100 ml)
GLB	1:0	0.06 ± 0.01	5.96
F1	1:1	0.15 ± 0.01	15.37
F2	1:2	0.27 ± 0.01	27.03
F3	1:4	0.30 ± 0.02	30.22
F4	1:8	0.41 ± 0.12	40.92
F5	2:1	0.43 ± 0.23	43.18

±Indicates SD (n = 3).

Figure 2. Dissolution profiles of LNCs compared with GLB. All data points represent the mean value (n = 3).

Table 3. Dissolution parameters of GLB and LNCs.

Batch	Q5min	Q10min	Q30min	Q60min	% DE60min	MDT (60 min)
GLB	0.36	0.71	1.15	1.47	21.09	46.89
F1	2.87	3.47	4.11	4.94	80.39	11.51
F2	0.60	1.02	1.87	2.70	52.52	28.30
F3	0.40	0.98	1.31	1.89	42.55	34.35
F4	0.44	1.02	1.60	1.83	40.27	35.62
F5	0.55	0.67	1.00	1.93	46.75	31.85

Q, Quantity of drug released at time.

Table 4. Particle size analysis data and ZP report of GLB and LNCs.

Batch	Z. avg (d nm)	Avg. ZP (mV)	PDI (avg.)
GLB	1551	−38.1 ± 0.2	0.417
F1	155	−51.7 ± 0.1	0.310
F2	710	−45.8 ± 1.3	0.309
F3	842	−48.4 ± 0.7	0.397
F4	227	−58.3 ± 0.5	0.431
F5	787	−48.0 ± 0.3	0.878

±Indicates SD (n = 3).

Figure 3. (A) X-ray diffraction spectra of GLB, PEG 20000, PM (1:1), and lecithin and (B) LNCs (F1–F5) at 2θ-scale.

Figure 4. (A) DSC thermograms of GLB, PEG 20000 and PM-1:1 and (B) LNCs.

Figure 5. FTIR spectra of GLB, PEG 20000 and PM-1:1 (A) and LNCs (F1–F5) and stabilized formulation (GLB-F1-S-O) after three months of storage.

Table 5. Stability analysis data of optimized NC (Batch F1).

		Observation (months)
Temp.	Parameters	0	1	2	3
3–5 °C ± 2	Physical appearance	Milky white	No change	No change	No change
	Drug content	50.08 ± 0.41	50.07 ± 0.20	50.04 ± 1.97	50.05 ± 0.31
20–25 °C ± 2	Physical appearance	Milky white	No change	No change	No change
	Drug content	50.08 ± 0.13	50.06 ± 1.98	49.71 ± 2.18	49.63 ± 0.35
37 °C (RH 75%)	Physical appearance	Milky white	No change	No change	No change
	Drug content	50.08 ± 1.01	50.05 ± 0.43	49.81 ± 1.30	49.76 ± 0.36

±Indicates SD (n = 3).

Figure 6. (A) SEM images of raw GLB, (B) non complexed F1 NCs, (C) aggregated NCs before complexation and after microscopical examination, (D) complexed F1 LNCs and (E) complexed F1 LNCs dispersed in water and air dried.

Table 6. RT and peak area of GLB and test sample.

Batch	Conc. (µg/ml)	RT	Peak AUC 1 h
GLB	19.8 ± 0.15	2.9 ± 0.55	392 706 ± 4303
Test sample (F1)	12.6 ± 0.25	2.7 ± 0.47	238 069 ± 1424
p value t test	p < 0.001	p > 0.05	p < 0.001

±Indicates SD (n = 3).

p ≤ 0.05, Statistical significant test was done by one-way ANOVA followed by student’s t-test.