Lipid-PLGA hybrid nanoparticles of paclitaxel: Preparation, characterization, in vitro and in vivo evaluation

Nanoprecipitation: Applications for Entrapping Active Molecules of Interest in Pharmaceutics

“…Regarding lipid nanoparticles, only systematic studies have been reported to aid in understanding the variables that influence the preparation of the carriers; among them, the contributions of Martínez-Acevedo et al [54] on the influence of the used recipe and Noriega-Pelaez [55] on the study of the particle preparation process are highlighted. Concerning the hybrid particles, research works to date have focused primarily on the impact of the starting materials on the particle characteristics [5,9,12,23,56].…”

“…To this end, rotary evaporation [14, 18, 22-24, 31, 55] and centrifugation [5, 6, 12, 13, 15, 16, 23, 25, 27-29, 36, 56, 57] are the most used methods; however, filtration [4,6,16,18,24] and dialysis [7-9, 21, 27, 34] have also been reported. Likewise, lyophilization is the preferred technique to stabilize the nanoparticles, although the storage to low temperatures has been used to preserve the aqueous dispersions [5,8,9,13,21,29].…”

“…For some active molecules such as methotrexate, N-acetylcysteine, psoralen, quercetin, and paclitaxel, the prolonged drug release could be related to the uniform distribution presumed for the drug into the matrix and the core-shell structure of the particle, which difficult the diffusion of the drug toward the release medium [9]. Likewise, the hydrolysis and erosion processes of the polymeric core could be hindered by the lipid layer surrounding the polymeric core [34] or, perhaps, the hydrophobic interactions of the active molecule with the polymer might result of relevance for the drug release [5]. These effects offset, for example, the favorable solubility gained because of the precipitation of amorphous active during the preparation of the particles, which is expected to facilitate the drug delivery [9].…”

“…Regarding the carriers prepared by nanoprecipitation, among the reported developments of particles that could theoretically allow them a better in vivo performance are: (i) particle sizes lesser than 100 nm for polymeric nanospheres [25,26,34], solid lipid nanoparticles [71], and hybrid nanoparticles [7,34,56], (ii) positively charged polymeric nanospheres by using chitosan [72] and Eudragit ® RL 100 [18] as polymers or positively charged hybrid nanoparticles prepared from lipids as the stearylamine [5], (iii) stealth polymeric nanospheres [17,27] and stealth hybrid particles [4][5][6][7][8], and (iv) targeted cancer hybrid particles [7,59].…”

“…Some of the research works undertaken during the last years have proposed the vectorization in nanoparticles, via nanoprecipitation, of hydrophobic active molecules, mainly exhibiting logP values higher than 3. They include antineoplastics (e.g., doxorubicin [4], paclitaxel [5,6], docetaxel [7,8], methotrexate [9], triptolide [6], cucurbitacin [10], and sorafenib [11]), antiretrovirals (e.g., efavirenz [12] and nevirapine [13]), immune suppressants (mycophenolate [14]), anti-inflammatories (clobetasol [15], fluticasone propionate [16], dexamethasone [17,18], and diclofenac [19]), antimicrobial and antifungal agents (polymyxin B [20], amphotericin B [21], itraconazole [22], and linezolid [23]), antihyperlipidemics (fenofibrate [24,25]), anesthetics (tetracaine [26] and ketamine [27]), antihypertensives (nimodipine [28] and atenolol [29]), vitamins or their precursors (β-carotene [30] and vitamin E [31]), and antioxidants (quercetin [14,32]). Likewise, although in a much smaller number, hydrophilic active molecules such alendronate [33], N-acetylcysteine [34], and calcein [35], have been investigated.…”