Preparation a core‐shell lipid/polymer nanoparticle containing Isotretinoin drug with pH sensitive property: A response surface methodology study

Abstract

In this study, a core‐shell lipid/polymer nanoparticle (NP) was prepared to deliver Isotretinoin drug with pH sensitive and controllable drug release property for oral administration usage. Chitosan was cross‐linked to tripolyphosphate to form the core of the NP using the ionic gelation technique and coated with glycerol monostearate lipid as a shell by applying a two‐step approach. Response surface methodology was used to investigate the effects of various parameters on particle size and drug entrapment efficiency of the nanoparticles. Optimal nanoparticles with lower particle size and higher entrapment efficiency had a diameter of 100 nm based on TEM analysis and 64% drug entrapment efficiency. Coating NPs surface with lipid changed the NPs charge, hydrophilicity and swelling property. Lipid coating NPs changed release rate from 6 to 4% after 2 h in simulated gastric fluid (SGF), 9 to 16% after 6 h in simulated intestine fluid (SIF) and 21 to 71% after 7 days in blood medium. Kinetic modeling of drug release confirmed Fickian diffusion based on Higuchi model in SIF and blood media where swelling and dissolution of polymer network were negligible, while drug dissolution due to polymer swelling in SGF media was the dominant mechanism for drug release.

Polymeric nanoparticles containing different oils as insecticides against the storage pest Tribolium castaneum (Herbst) (Coleoptera: Tenebrionidae)

“…In other words, increasing the CS polymer concentration to cross‐linker ratio in the solution enhances the particle size. This observation is also cross‐validated with the other findings 45–47 …”

Dual‐drug delivery of sodium ceftriaxone and metronidazole by applying salt‐assisted chitosan nanoparticles: Stability, drug release, and time‐kill assay study against Bacteroides fragilis

“…The particle sizes obtained by TEM are approximately 212 ± 31, 238 ± 28, and 276 ± 21 nm for CTX‐loaded, MTZ‐loaded, and CTX‐MTZ loaded CS NPs, respectively. The larger particle size obtained from DLS analysis is likely related to the swelling property of CS in the hydrous medium 46,49 …”

“…As a result, the release of CTX/MTZ drug from both nanostructures follows the Korsmeyer‐Peppas model. In this model, if n < 0.49, the release mechanism is Fickian diffusion; if 0.49 < n < 0.89, the dominant mechanism is the degradation of polymer network and non‐Fickian diffusion, and if n = 0.89, the release is time independent 46,47 . According to the n values for CTX and MTZ of ( n = 0.2979, 0.3022, 0.3473 for S1, S2 and S3) and ( n = 0.9624,0.976, 0.9729 for S1, S2 and S3), respectively, the dominant mechanism is Fickian diffusion, in which swelling and decomposition of the polymer network are negligible.…”

“…Several kinetic models, including the zero‐order, first‐order, Higuchi, and Korsmeyer‐Peppas models, were utilized to examine the in‐vitro drug release patterns. Table 1 displays the equations and parameters for each model 46,47 …”

“…The larger particle size obtained from DLS analysis is likely related to the swelling property of CS in the hydrous medium. 46,49 Fourier transform infrared spectrum, XRD pattern, TGA diagram and BET analysis of CS, CTX, MTZ, and salt-assisted CTX-MTZ-loaded CS NPs are shown in Figure 2. Characteristic peaks in the FTIR spectrum of CS, CTX, and MTZ are presented in Table 3.…”