Spray-Dried Silica Xerogel Nanoparticles as a Promising Gastroretentive Carrier System for the Management of Chemotherapy-Induced Nausea and Vomiting

Figures & data

Table 1 The Composition (Molar Ratio) and the Physicochemical Properties of the Investigated (GR/CHL)-Loaded Spray Dried SXNs (Mean ± S.D., n = 3)

System	TEOS: Water: Acetic Acid (Molar Ratio)	Physicochemical Properties									Desirability Values
		Size (nm)	PDI	Zeta Potential (mV)	CHL			GR
					EE (%)	P1h (%)	P8h (%)	EE (%)	P1h (%)	P8h (%)
SXN1	1:15:0.5	143.80 ± 6.71	0.13 ± 0.02	−5.59 ± 0.22	42.16 ± 1.94	15.23 ±2.10	53.97 ± 6.12	72.15 ± 1.94	19.08 ± 5.21	93.25 ± 5.20	0.62
SXN2	1:15:1.0	211.81 ± 16.19	0.18 ± 0.01	−5.23 ± 0.14	45.10 ± 0.39	21.04 ± 6.31	64.14 ± 4.21	70.46 ± 0.16	27.89 ± 6.22	98.80 ± 4.41	0.61
SXN3	1:15:1.5	465.41 ± 36.91	0.35 ± 0.06	−5.25 ± 0.34	52.47 ± 1.54	20.14 ± 4.24	64.16 ± 6.24	69.83 ± 3.16	30.24 ± 8.25	98.06 ± 3.14	0.36
SXN4	1:20:0.5	181.63 ± 7.82	0.22 ± 0.03	−5.18 ± 0.34	59.39 ± 1.97	22.75 ± 7.57	60.36 ± 5.19	73.94 ± 1.58	30.74 ± 9.34	99.33 ± 1.47	0.69
SXN5	1:20:1.0	242.66 ± 17.82	0.24 ± 0.01	−3.10 ± 0.19	62.17 ± 2.35	27.14 ± 9.70	69.38 ± 7.46	71.49 ± 0.29	36.24 ± 6.19	98.36 ± 1.97	0.64
SXN6	1:20:1.5	502.43 ± 19.45	0.48 ± 0.04	−4.27 ± 0.20	57.17 ± 1.93	30.97 ± 6.25	73.25 ± 6.49	74.50 ± 1.38	39.47 ± 7.91	98.87 ± 4.71	0.36
SXN7	1:25:0.5	127.45 ± 13.52	0.14 ± 0.04	−4.89 ± 0.74	71.67 ± 1.38	35.95 ± 6.93	60.58 ± 5.18	82.42 ± 2.18	40.97 ± 9.31	98.70 ± 3.13	0.64
SXN8	1:25:1.0	141.82 ± 9.56	0.28 ± 0.06	−4.97 ± 0.94	69.41 ± 1.42	38.71 ± 8.12	72.00 ± 4.59	84.57 ± 1.74	51.61 ± 9.50	99.07 ± 2.12	0.51
SXN9	1:25:1.5	347.16 ± 15.23	0.42 ± 0.07	−5.17 ± 0.64	72.87 ± 0.82	49.13 ± 5.69	85.18 ± 3.16	87.18 ± 0.98	60.24 ± 8.66	99.70 ± 1.56	0.22

Figure 1 The in vitro release profile of CHL from SXNs, in comparison to an aqueous CHL suspension, in 0.1N HCl at 37 ± 0.5 °C (mean ± SD, n=3).

Figure 2 The in vitro release profile of GR from SXNs, in comparison to an aqueous GR solution, in 0.1N HCl at 37 ± 0.5 °C (mean ± SD, n=3).

Figure 3 A scaning electron micrograph of SXN4.

Figure 4 Pore size distribution of (GR/CHL)-loaded SXN4.

Figure 5 Photographs taken before and during in vitro wetting and floating studies of (GR/CHL)-loaded SXN4 showing the wetting time in 0.1 N HCl at 37 ± 0.5°C.

Table 2 The Estimated Pharmacokinetic Parameters of GR and CHL Following Oral Administration of SXN4 and an Aqueous CHL Suspension Containing GR in Fasted Rats (Mean ± S.D., n = 6)

Pharmacokinetic Parameters	CHL		GR
	Suspension	SXN4	Solution	SXN4
Cmax (ng/mL)	137.82 ± 15.17	682.51 ± 22.37	8.10 ± 1.23	10.90 ± 1.11
*Tmax (h)	4 (2–4)	2 (1.5–3)	2 (1–2)	3 (1–3)
MRT(0-∞)(h)	2.51 ± 0.19	6.72 ± 1.49	4.57 ± 0.94	9.39 ± 1.94
AUC(0–24) (ng·h/mL)	816.7 ± 20.14	1435.35 ± 19.52	30.65 ± 9.75	54.59 ± 14.29
AUC(0-∞) (ng·h/mL)	905.1 ± 22.62	1442.15 ± 32.76	32.31 ± 8.64	60.23 ± 4.97

Note: *Median (range).

Figure 6 (A) Plasma concentration-time curves of CHL from SXN4 and an aqueous CHL suspension following oral administration in fasted rats at 4 mg/mL doses, mean ± S.D., n = 6. (B) Plasma concentration-time curves of GR from SXN4 and an aqueous GR solution following oral administration in fasted rats at 2 mg/mL doses, mean ± S.D., n = 6.