Atazanavir-loaded Eudragit RL 100 nanoparticles to improve oral bioavailability: optimization and in vitro/in vivo appraisal

Figures & data

Table 1. Preparation of ATV NPs as per the experimental design.

	Coded factor levels
Trial no.	Factor 1, Polymer (mg)	Factor 2, surfactant (mg)
1.	0.00 (200)	0.00 (200)
2.	0.00 (200)	1.00 (300)
3.	−1.00 (100)	1.00 (300)
4.	−1.00 (100)	−1.00 (100)
5.	0.00 (200)	0.00 (200)
6.	1.00 (300)	−1.00 (100)
7.	−1.00 (100)	0.00 (200)
8.	0.00 (200)	0.00 (200)
9.	1.00 (300)	0.00 (200)
10.	0.00 (200)	−1.00 (100)
11.	1.00 (300)	1.00 (300)
12.	0.00 (200)	0.00 (200)
13.	0.00 (200)	0.00 (200)

Figure 1. Response surface plot showing the influence of TTAB (surfactant) and Eudragit RL 100 (polymer) on (A) particle size (D_nm), (B) drug encapsulation efficiency (D_EE) and (C) mean percent drug release in 24 h (%Rel_24h) for NPs formulations of ATV.

Figure 2. In vitro release profile of ATV loaded Eudragit RL 100 NPs with TTAB as surfactant in pH 7.4 phosphate buffer. Data points shown are mean ± standard deviation (SD) (n = 3).

Figure 3. TEM image shows particle size of OPT formulation.

Figure 4. Plasma drug level profiles of pure drug and OPT formulation. Each point represents mean of six replicates and each cross bar indicates 1 SEM.

Figure 5. Percent increase in permeability parameters and absorption parameters in OPT formulation vis-à-vis pure drug using in situ single pass intestinal perfusion technique.

Table 2. Various parameters of the OPT formulation analyzed at different time points during stability studies.

Time (month)	Dnm	% DEE	%Rel24 h	ζ potential
25 °C ± 2 °C/60% RH ± 5% RH
0	465.59	59.28	89.33	+24.53
1	464.71	59.12	89.01	+24.37
3	464.23	58.83	88.76	+24.19
6	463.82	57.96	87.43	+23.88