*Nanoprecipitation: Applications for Entrapping Active Molecules of Interest in Pharmaceutics DOI: http://dx.doi.org/10.5772/intechopen.93338*

**Table 5.**

 *Summary of experimental conditions and general results reported in research works on efficacy testing*

 *of* 

*nanoparticles*

 *prepared by the* 

*nanoprecipitation*

 *technique.*

**Nanoparticle**

**126**

**Assay**

*In vivo*

antitumor

Sprague-Dawley

 rats

 25 mg/kg

 30 days

 Tumor width, length, and

size

Combination

QC loaded LPN

significant suppression growth as compared to other

groups.

*Nano- and Microencapsulation - Techniques and Applications*

Combination

nanoparticles

shows significantly effect compared with individual

nanopreparation

 (MPA-NP and QC-

NP).

 (MPA-NP + QC-NP)

 higher cytotoxic

 treatment of

 therapy of MPA and

demonstrates

 of tumor

efficacy

Cytotoxicity

MCF-7 human breast

10, 20, 40, and

nr.

Optical density

> 60 μg/mL

cancer cell

(MTT assay)

> HNP (quercetin)

 Cellular

Caco-2 cells

25 mg/kg

 0.5 h

CLSM

Excellent affinity and

to enterocytes

 allows HNP to be

efficiently transported.

permeability

[32]

internalization

Cytotoxic

Lymphoblastic

 leukemia

5, 10, and 20 μM

 24 h

Spectrophotometry

 UV

 HNP have higher cellular

approachability

with the cellular uptake by Caco-2

 that accords well

cells.

P388 cells

evaluation on

P388 cells (MTT

assay)

*In vivo*

DBA/2 mice

25 mg/kg

 21 days

 Automatic blood counter

 HNP can enhance the oral

bioavailability

 of QC.

antileukemic

effect

HNP (paclitaxel)

 Plasma protein

Blood sample from a

0.7 mg/mL

 2 h

Bradford assay

 The protein binding of HNP was

[5]

found between 15.1 and 33.7%. The

interaction between the biological

environment

controlled by surfactant.

 and HNP can be

healthy volunteer

binding study

**Cellular/animal**

 **model Drug** 

**Experimental**

 **conditions**

 **for efficacy testing**

**concentration**

 **Time of**

**Technique**

 **of analysis**

**interaction**

**—cellular**

**model**

**General results**

nanoparticles give good results in this sense. First, the incorporation of the active molecules into the carriers preserve the anticancer activity [9] and nanoparticles offer better performance compared with the free drug [4, 14, 56], in some cases being dose dependent [6, 8, 11]. Besides, significant improvements in the *in vivo* anticancer performance were achieved by the encapsulation of both an anticancer molecule (mycophenolate) and an antioxidant agent (quercetin) into the same hybrid nanoparticle, as quercetin prevents mycophenolate of its hepatic metabolism via the oxygenase enzymes [14]. Moreover, it was demonstrated that the *in vivo* tumor treatment in mice prolongs the life of the animals [7].

Taken advantage of the slow-release patterns that could be obtained with nanoparticulated systems, the development of carriers exhibiting antimicrobial and anesthetic activities are also of interest in research. Thus, the lowest values of minimum inhibitory concentrations of SLN containing polymyxin B or amphotericin B [20, 21] with respect to the free drugs contribute to support the applicability of nanoparticles prepared by nanoprecipitation in this area. In line with this, polymeric nanoparticles containing Brazilian red propolis extract have also shown antileishmanial activity [36], and linezolid-loaded hybrid nanoparticles demonstrated their ability to be retained in biofilms optimizing their antibacterial performance [23]. Regarding the behavior of nanoparticles in anesthetic and antiinflammatory tests, tetracaine-loaded SLN exhibited prolonged antinociceptive effect leading to better control of pain [26].

Finally, the possibilities to get target particles prepared by the nanoprecipitation technique have been opened from the research works of Jeannot et al. [59] and Dehaini et al. [7] who investigate hyaluronan and folate as receptors chemically bonded to the polymer obtaining promising results for cancer therapies.

#### **6. Conclusions**

Nanoprecipitation is a simple, energy-efficient, and versatile method to entrap active molecules into carriers at the submicron and nanometric levels being the most common developments those oriented to obtain polymer, lipid, and hybrid particles. As the knowledge on the *in vivo* behavior of nanocarriers progresses and the need to produce them at the industrial scale demands for greater efficiency, the technique and the used starting materials have been optimized to improve the characteristics of the carriers and the control and standardization of continuous processes. In this way, sophisticated devices have been proposed to get sizes lower than 100 nm and the procedure has been refined, either through the chemical modification of polymers or through the careful definition of the work conditions, leading to particles entrapping hydrophobic and hydrophilic molecules, or exhibiting a targeted performance, a positive charge on their surface, or behaviors as stealth carriers. Moreover, the hybrid nanoparticles are promising drug delivery systems where the advantages of both polymeric and lipid particles are harnessed in their design to offer major drug loadings, slow drug-release patterns, and better pharmacokinetic properties. Regardless of the type of carrier, nanoprecipitation seems to be appropriate to obtain safe particles. Even using solvents characterized by inherent toxicity, the satisfactory results achieved by safety tests support their applicability in pharmaceutics. On this basis, it is expected that research on nanoprecipitation will continue looking for innovative solutions to the challenges facing current and future medicine. Some of the findings reported by different research teams and summarized in this chapter provide valuable insights regarding the potentialities of this technique in this respect.

**Author details**

**129**

Oscar Iván Martínez-Muñoz, Luis Fernando Ospina-Giraldo

\*Address all correspondence to: cemorah@unal.edu.co

Departamento de Farmacia, Facultad de Ciencias, Universidad Nacional de

*Nanoprecipitation: Applications for Entrapping Active Molecules of Interest in Pharmaceutics*

*DOI: http://dx.doi.org/10.5772/intechopen.93338*

© 2020 The Author(s). Licensee IntechOpen. This chapter is distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/ by/3.0), which permits unrestricted use, distribution, and reproduction in any medium,

and Claudia Elizabeth Mora-Huertas\*

Colombia Sede Bogotá, Bogotá, Colombia

provided the original work is properly cited.

*Nanoprecipitation: Applications for Entrapping Active Molecules of Interest in Pharmaceutics DOI: http://dx.doi.org/10.5772/intechopen.93338*
