It was shown that the amount of water required to prepare a proper wet mass was affected by composition of formulations.
Reconstructed human skin is also an unbeatable tool for screening and assessing the efficacy of new active ingredients, deciphering their mechanism of action, and, finally, optimizing the composition of formulations to maximize in vivo benefits.
To more precisely understand how the composition of formulations affected the cell internalization of the NPs, H22 cells were incubated with the coumarin-6-PLA NPs/MMC-SPC and coumarin-6-PLA NPs/MMC and subsequently analyzed the cells by flow cytometry.
The composition of formulations is given in Table 1.
Table 1 shows that differences in composition of formulations A, B, and C are only in the amount of water used to dissolve the peptide in the O/W primary emulsion.
Passive strategies encompass the proper selection of the composition of the formulation, zeta potential, particle size and preparation method.
The composition of optimal formulation was determined as 0.69% (w/v) lipid and 26.64% (w/w) drug/lipid ratio.
On the basis of optimization criteria, composition of optimized formulation F0 (Methocel K100LV = 77.98 mg and Carbopol 934 = 82.02 mg) was determined by statistical analysis.
The optimized composition of SNEDDS formulation was 25% v/v Oleoyl polyoxyl-6 glycerides, 37% v/v Tween 80, 38% v/v diethylene glycol monoethyl ether, and 3% w/v PPK.
The composition of optimized formulation was Sefsol 218 (20% w/w), Tween 80 (18% w/w), Carbitol (18% w/w) and standard buffer solution pH 5 (44% w/w) as oil, surfactant, cosurfactant and aqueous phase, respectively, containing 5 mg of ramipril showing drug release (95%), droplet size (80.9 nm), polydispersity (0.271), viscosity (10.68 cP), and infinite dilution capability.
