Review

Nanoemulsions and dermatological diseases: contributions

and therapeutic advances
^ bo de Souza, MsC, Douglas Dourado Oliveira, Bs, Neila de Paula Pereira, PhD,
Myla Lo
and Denis Melo Soares, PhD

Department of medicament, Pharmacy Abstract

Faculty, Federal University of Bahia, Skin disease is one of the most common human diseases and affects between 30% and
Salvador, Bahia, Brazil
70% of individuals, which requires a lot of attention to their treatments. The delivery of
Correspondence
active pharmacological ingredients at the topical level is a challenge because of the
Myla Lo^bo de Souza, MsC difficulties in overcoming the mechanical barrier created by the skin and reaching greater
Department of medicament, Pharmacy depths, since delivery specificities are decisive for the degree of effectiveness. In this way,
Faculty, Federal University of the nanoemulsions emerge as a potential system for the incorporation of active substances
Bahia Salvador
in the cells and for the controlled release of active principles. The present article intends to
Bahia
review the main treatments for which the nanoemulsions were used in the field of
Brazil
E-mail: myla@ufba.br & dermatology. In addition, it discusses the results and advantages over the other
mylobo.souza@gmail.com dermatological therapies that are being used. The results showed that the particle size in
nanoemulsions increased the contact surface area, resulting in increased drug efficacy,
Funding: None. even in comparison with other existing pharmaceutical formulations. In conclusion, it has
been shown that nanoemulsions have a better performance in efficacy, safety, permeability
Conflict of interest: None.
profile, and bioavailability compared with other formulations studied.
doi: 10.1111/ijd.14028

migration of the active principles through the skin, playing a

Introduction
Nanoscience and nanotechnology have been recognized as a
key trend in science and technology in the 21st century.1 There-
fore, they are being studied and applied in distinct areas, such
as chemistry, physics, biology, engineering, information, and
even diverse areas of health. Nanotechnology is based on the
ability to characterize, manipulate, and organize materials on a
nanoscale, which gives the products characteristics and behav-
iors different to those found at the larger scale.2 In this context,
we find innumerous areas where nanotechnology can offer a
significant contribution, such as in the case of dermatology.
Skin is the largest organ of the human body, responsible,
among other functions, for the protection of the organism
against external aggression, being the physical barrier against
the penetration by environmental particles and microorgan-
isms.3 Structurally, it is divided into three layers: the hypoder-
mis, which connects the skin to the deeper structures such as
muscles and bones; the dermis, which possesses a great vari-
ety of types of cells, nerves, and blood and lymphatic vessels
surrounded by connective tissue; and the epidermis, the most
external layer, which stands out in its role as barrier, essentially
determined by one of its constituents, the stratum corneum.4 In
this manner, it is the epidermis which determines the depth of
more significant role as an obstacle to penetration, which will be
the limiting factor of this process. The delivery of active com-
pounds at the topical level is a challenge given the difficulties in
overcoming the mechanical barrier presented by the skin.3,4
Therefore, the transport system for the medication is one of the
determining factors in terms of reaching the intended target
layer. A deeper penetration and the specifics of delivery are
important for the degree of effectiveness of the nanoformulated
substances.5 Therefore, nanoformulated medications emerge as
an excellent strategy to exercise a controlled and directed deliv-
ery of the active principals, with deeper reach.
With the aim of achieving a successful topical application and
liberation of the active principles, a wide variety of nanostruc-
tures are being developed.6,7 Of these systems, nanoemulsions
have evolved as a potential system of drug administration due
to their capacity to penetrate the deeper skin layers (Fig. 1).
Nanoemulsions are very fine dispersions, formed by the con-
junction of two immiscible substances – normally water and oil –
where one of the liquids is distributed throughout the other,
whose globule size is, on a nanometric scale, specifically
around 20–500 nm. Their appearance can be transparent or
milky, depending on the size of the globule, tending toward
greater transparency the smaller the size – normally less than
1

ª 2018 The International Society of Dermatology International Journal of Dermatology 2018

2 Review Nanoemulsions and dermatological diseases
Figure 1 Permeation of normal products versus nanoemulsions (Adapted from Mano42)
200 nm.8 They are systems with kinetic stability, which is
directly related to the preparation, due to its using nonionic and/
or polymer tensoactive principles and by reducing the size of
the globules, whose Brownian motion reduces the action of the
force of gravity, therefore preventing the phenomena of instabil-
ity.7,8 Consequently, we can avoid the creation of sediments
and flocculation during the storage of the product, which will
maintain the system dispersed, without separation of the
phases and with good longevity.
The main use of nanoemulsions is principally directed toward
the incorporation of active substances in the cells, for the con-
trolled liberation of active principles, as well as for the possibility
8,9
of uniting two immiscible substances in the same formulation
In the field of dermatology, they offer a number of advan-
tages, including low irritation of the skin, high permeability, and
a high capacity for carrying active substances when compared
with other nanostructures, given that these can transport com-
pounds deeper into the skin at more elevated concentrations.8
In addition, they also possess advantages in relation to other
administration means, such as oral and parenteral, including
greater safety and control of the dose, patient adherence to the
treatment, and avoidance of first-pass metabolism. In fact,
nanoemulsion delivery systems have the potential to become
an effective, safe, and well-accepted delivery system for topical
lipophilic drugs.
Among the many nanostructured carriers, the nanoemulsions
exhibit interesting characteristics when compared with other
systems, especially regarding dermatological application. In the
case of solid lipid nanoparticles, they have a lower capacity to
maintain the encapsulation of the active substances, and there
may be the formation of alternative colloidal structures and
physical instability during storage or administration due to the
complexity of the lipid physical state.10 In addition, when main-
taining encapsulation, they tend to reduce and prolong the
release of the entrapped drug over several days or weeks,
International Journal of Dermatology 2018
de Souza et al.
which may not be adequate for many conditions of nonchronic
diseases.11,12 On the other hand, the liposomes present as car-
riers susceptible to the oxidative degradation of the phospho-
lipids in their composition, have low solubility, experience loss
of activity during the encapsulation, have a high cost of produc-
tion,13 and still have difficulty releasing assets, which involve
endocytosis, cell fusion, or lipid exchange.14 In this context, the
nanoemulsions are promising because they are easier to obtain,
have better kinetic stability, and have better solubilization of
active substances and high permeability and carrying capacity
of substances with higher flow of active release and higher pen-
etration.15–17 In addition, emulsified products such as nanoemul-
. sions are the most used for dermatological treatments because
of the good acceptance by consumers, because they have an
attractive appearance, are very pleasant to the touch, and their
composition resembles the hydrolipidic mantle that protects the
skin.18
Taking this into account, the present article seeks to examine
the main applications in which the nanoemulsions were
employed for dermatological treatments. In addition, we
intended to find which results and advantages compared to the
other dermatological therapies that are being used for these
pathologies and how the nanoemulsions can benefit these treat-
ments.
Main applications
Skin problems and diseases are extremely common worldwide
and, because of their visibility, often result in severe distress
and stigma for patients.19 At the global level, skin conditions
were the fourth leading cause of nonfatal disease burden.
Based on past results, the impact of these diseases is enor-
mous in high- and low-income countries. These results strongly
advocate the prevention and treatment of skin diseases in
future global health strategies as a matter of urgency.20 Among
ª 2018 The International Society of Dermatology
de Souza et al. Nanoemulsions and dermatological diseases Review 3

the major dermatological diseases affecting the general popula-
tion are hyperpigmenting diseases such as melasma, immune
diseases such as urticaria and dermatitis, inflammatory dis-
eases such as acne and psoriasis, infectious diseases caused
by fungi, viruses, and bacteria, as well as skin cancer.21 There-
fore, treatments that cover some of these major dermatological
pathologies, such as antimicrobial, antifungal, anti-inflammatory,
and anticancer treatments have been chosen for this article.
Due to the nanotechnology to allow better performance and effi-
cacy of the drugs, the nanoemulsions were the formulations
evaluated in the mentioned dermatological treatments.
Table 1 shows the articles used in this review that report the
use of nanoemulsions for the treatment of dermatological dis-
eases.
Antimicrobial activity
Wounds are inevitable events in life that can occur due to
unavoidable lesions, which can lead to infection of the skin by
diverse microorganisms, from usual skin microbiota to bacteria,
fungi, and protozoa found in the environment. Infected wounds
not adequately treated can lead to various inflammatory pro-
cesses such as cellulite and, in more serious cases, even bac-
teremia and septicemia.22 Therefore, the treatment of this
immediate condition uses antimicrobials. However, the increase
in resistance to this class of medications is a big problem that
needs to be resolved for the efficient management of these
infections.
The development of medications with alternative distribution
systems, such as nanoemulsions, has increased in recent years

Table 1 Studies that evaluated nanoemulsions for dermatological treatments, compared with other formulations

Pharmacological
Active principle activity Comparison References

Chlorhexidine Antimicrobial Chlorhexidine nanoemulsion versus Song et al26

chlorhexidine in solution
NB-201 and NB-402 Antimicrobial NB-201 and NB-402 versus nanoemulsion Dolgachev et al25
vehicle or saline
NB-201 Antimicrobial NB-201 versus placebo or Mafenide Acetate Hemmila et al24
(Sulfamylon) or sterile saline
Eucalyptus oil Antimicrobial Eucalyptus nanoemulsion versus control Sugumar et al22
versus neomycin
Neem (Azadirachta indica) Antimicrobial Neem nanoemulsion versus commercially Jerobin et al23
available tetracycline or oil neem
Amphotericin B Antifungal Amphotericin B nanoemulsion versus Hussain et al29
liposomal amphotericin B (Fungisome)
Amphotericin B Antifungal Amphotericin B nanoemulsion versus Hussain et al30
amphotericin B solution or Fungisome
Nystatin Antifungal Nystatin nanoemulsion versus ointment ndez et al28
Ferna
nystatin (Mycostatin)
NB-002 Antifungal NB-002 versus amphotericin B, ciclopirox, Pannu et al27
itraconazole, terbinafine, tolnaftate, and
naftifine
Clotrimazole Antifungal Clotrimazole nanoemulsion versus plain drug Kassem et al31
Flavanones isolated from Anti-inflammatory Flavones in solution versus flavones in Domınguez-Villegas et al35
Eysenhardtia platycarpa leaves nanoemulsion
Delta, alpha, and gamma tocopherol Anti-inflammatory Delta, alpha, and gamma tocopherol Fonghsu et al32
Suspension versus delta, alpha, and gamma
tocopherol nanoemulsion
Oleanolic acid and ursolic acid Anti-inflammatory Oleanolic acid and ursolic acid versus mixture Alvarado et al34
oleanolic acid and ursolic acid nanoemulsion
Meloxicam Anti-inflammatory Meloxicam nanoemulsion versus meloxicam Khurana et al33
solution
Foscan: tetra Anticancer: skin cancer Foscan nanoemulsion versus Foscan Primo et al37
(m-hydroxyphenyl) chlorin (m-THPC) homogeneous organic medium
Dacarbazine Anticancer: melanoma Dacarbazine suspensions versus Tagne et al39
Dacarbazine nanoemulsion
Daunorubicin Anticancer: melanoma Daunorubicin commercial versus Contente et al41
Daunorubicin nanoemulsion
Dacarbazine Anticancer: epidermoid Dacarbazine suspension versus dacarbazine Kakumanu et al40
carcinoma nanoemulsion
Acai oil Anticancer: melanoma Acai oil nanoemulsion versus phosphate Monge-Fuentes et al38
buffered saline

ª 2018 The International Society of Dermatology International Journal of Dermatology 2018

4 Review Nanoemulsions and dermatological diseases
and gained space in the treatment of recent bacterial infections,
given that they are used for the delivery of drugs to the
intended destination, generally without collateral effects.23 In
addition, they possess a greater bioavailability, lower toxicity,
physical stability, reach a greater surface area, and have
greater efficacy. A study undertaken in 2014, which assessed a
nanoemulsion with a eucalyptus oil base for antibacterial activity
in a Staphylococcus Aureus culture, showed a total loss of bac-
terial viability within 15 minutes of interaction with the formula-
tion, the opposite of the control in which there was no
bactericidal action.22 In addition, in the cutaneous irritation tests
and for scarring made on rats, there was no irritation of the
skin, and scarring was faster than in the animals treated with
neomycin, demonstrating that the eucalyptus oil nanoemulsion
possesses rapid bactericidal and scarring action, being rela-
tively toxic for S. aureus.
Another study, which sought to assess the antibacterial activ-
ity of a nanoemulsion with a vegetable oil base, tested neem oil
(Azadirachta indica) against the Vibrio vulnificus bacteria and
evaluated toxicity in vitro of this nanoemulsion in a human lym-
phocyte culture.23 The authors reported that the antibacterial
activity of this oil against V. vulnificus in previous experiments
possessed a minimal inhibitory concentration (MIC) of 6 mg/mL,
but the nanoemulsion developed with the neem oil base in this
study showed an MIC below 150 lg/mL. The cells treated with
the nanoemulsion showed both rupturing and disintegration of
bacterial cell wall and a significant alteration in the morphologi-
cal structure, to the contrary of those not treated, which were
found intact. Regarding cytotoxicity, Jerobin et al.23 demon-
strated that a significant reduction of the cellular viability of the
lymphocytes in vitro was not observed in concentrations of the
substance up to 1.2 mg/mL (approximately 10 times the MIC).
Therefore, the study showed that the nanoemulsion tested can
be used as an effective antibacterial agent in the treatment of
V. vulnificus infections without toxicity in human lymphocytes at
concentrations up to 10 times MIC approximately.
Nanoemulsions containing antimicrobial agents have also
been studied for the treatment of burns, given the necessity to
develop a new generation of broad spectrum, topical antimicro-
bial agents that can penetrate deeply into the burn wound.
Hemilla et al.24 tested an innovative antimicrobial nanoemulsion
(NB-201) in the treatment of burn wounds with the objective of
attenuating the development of infection by Pseudomonas
aeruginosa and diminishing dermal inflammation in a test animal
with partial lesion. The results showed a reduction in bacterial
count in the skin treated with NB-201, where 3 of the 23 ani-
mals demonstrated a level of infection of the wound, while 29 of
32 animals in the control group exhibited infection, with no sta-
tistical difference in terms of the treatment with standard antimi-
crobials. Beyond this, the nanoemulsion reduced the dermal
level of inflammatory cytokines and infiltration of neutrophils in
the wound, showing that NB-201 was effective for use in burn
wounds.
International Journal of Dermatology 2018
de Souza et al.
These outcomes are also confirmed in the study by Dol-
gachev et al.,25 which investigated the antimicrobial efficacy of
two different nanoemulsions (NB-201 and NB-402) against
Gram-positive and Gram-negative bacteria (Staphylococcus
aureus and Pseudomonas aeruginosa) in a model burn in
rodents. Both formulations significantly reduced infections in
burn wounds and diminished the count in at least three cycle
logs, when compared with the control. They also diminished the
dermal recruitment of neutrophils and proinflammatory cytoki-
nes, suppressing progression of the burn wound 72 hours after
lesion.
Good treatment results for burns using nanoemulsions were
also found in a study carried out in China, in which a chlorhexi-
dine nanoemulsion had a better and faster action against methi-
cillin-resistant Staphylococcus aureus (MRSA) in an in vitro and
in vivo burn model, in comparison with the chlorhexidine in solu-
tion.26 There was also a better effect in the inhibition of the for-
mation of the biofilm and in its elimination. Therefore, the
nanostructured formulation conferred better antibacterial and
antibiofilm activity against the infected burn wounds than the
common formulation.
Such complementary results suggest that the size of the par-
ticles in nanoemulsions increase the surface area, which can
result in greater interaction with bacterial membranes, therefore
resulting in an increase in the antibacterial activity of the medi-
cations.24,25
Antifungal activity
Superficial fungal infections are found in the upper layers of the
skin and mucous membranes, for hair and nails, and are one of
the main reasons for visiting a dermatologist. The majority of
them are treated with topical antifungals and/or oral therapies,
frequently associated with an antifungal and a corticosteroid to
rapidly reduce inflammatory symptoms and increase the
bioavailability of the antifungal agent.27 With candidiasis being
one of the most well-known fungal infections, a study carried
out in 2013 had as its main objective to assess nanoemulsions
with a nystatin base ideal for topical treatment.28 The assays
showed that the nanoemulsion had a quicker effect than the
commercial nystatin cream, that the substance was not
absorbed into the systemic circulation, and that the quantity
retained on the skin was sufficient to guarantee antifungal activ-
ity, which was greater for the nanoemulsion. The results
showed that nystatin in the form of a nanoemulsion was more
effective due to greater permeation of the skin without toxic
effects. Another study that also sought to develop a stable for-
mulation, with antifungal activity and without adverse systemic
effects, developed a topical nanoemulsion with a B ampho-
tericin base as an alternative means of administration, given
that the standard manner possesses many toxic effects.29 In
vitro permeation tests showed that the nanoemulsion had a lib-
eration profile of the substance 12 times greater than the com-
mercial presentation (nanoencapsulated cream), just as the
ª 2018 The International Society of Dermatology
de Souza et al.
ex vivo tests showed better cutaneous permeation. In addition,
the in vivo investigation of the biological and hematological mar-
ker parameters did not result in significant nephrotoxicity, show-
ing it to be not only more effective but also safer. Another
recent study, conducted by the same author, evaluated the
influence of lipids and surfactants added to nanoemulsions on
the antifungal activity against Candida albicans and Aspergillus
fumigatus.30 In the evaluation of the ex vivo assay, it exhibited
sustained release and an improved flow value compared with
the same drug solution, without showing toxicity. In vivo, they
showed increased antifungal activity, which could be related to
MIC reduction. Thus, the explored excipients greatly affect drug
penetration, demonstrating potential for enhanced permeation
and the important role of nanoemulsions to enhance drug per-
meation.
Positive results with nanoemulsions were also found in the
study by Kassem et al.,31 whose aim was to prepare a
nanoemulsion with a clotrimazole base, seeking to increase its
solubility and, consequently, its absorption profile. The
researchers concluded that the immediate liberation profile of
the substance confers a good bioavailability profile on the
nanoemulsion, suggesting a better absorption of clotrimazole.
Seeking to assess the activity of antifungal substances in
nanoemulsions, researchers compared the compound NB-002
(a nanoemulsion with an antifungal base) with antifungal drugs
already available for treatment against the main dermatophytes
responsible for cutaneous infections (Trichophyton rubrum,
Trichophyton mentagrophytes, Trichophyton tonsurans, Epi-
dermo-phyton floccosum, and Microsporum spp.), as well as 12
other genus of filamentous fungi.27 NB-002 was the only one
that presented fungicidal activity against all the dermatophytes
tested, when compared with the commercial antifungals (am-
photericin B, ciclopirox, itraconazole, terbinafine, tolnaftate, and
naftifine), as much in topical as in oral use, including against
Candida albicans-resistant species. In relation to other filamen-
tous fungi, 10 of the 12 isolated were susceptible to a concen-
tration of ≤4 lg/mL of NB-002, distinguishing it from the
commercial options by its potency.
In summary, antifungals in the form of nanoemulsions have
generated good results in terms of efficacy, safety, permeation
profile, and bioavailability, including when compared with the
formulation of other already existing pharmaceutical formula-
tions.27–29
Anti-inflammatory activity
Inflammation is the first immune response of the body when
infected or irritated by an external aggression. Inflammation is
associated with the normal process of healing. The mechanisms
involved in this process are complex and when they are not well
regulated can result in inflammatory diseases.23 A study had as
its objective the comparison of the anti-inflammatory properties
of suspensions containing different isomers of tocopherol with
its formulation in nanoemulsions, observing bioavailability.32
ª 2018 The International Society of Dermatology
Nanoemulsions and dermatological diseases Review 5
Inflammation, assessed by auricular thickness in rats, was sig-
nificantly reduced by the nanoemulsion (up to 70%) in relation
to the control and suspension, where there was no reduction. In
addition, bioavailability was 2.4 times greater than the suspen-
sion, indicating that the formulation in nanoemulsion had better
anti-inflammatory properties than the suspensions of these com-
pounds.
With the aim of guaranteeing products with a greater capacity
for controlled and sustained liberation, researchers assessed
the permeation and deposition on the skin by ex vivo test, anti-
inflammatory activity and toxicity in vivo of the nanoemulsion
with a meloxicam gel base in comparison with the formulation in
solution.33 Percutaneous permeation tests showed a permeation
three times greater of meloxicam in the gel nanoemulsion than
in solution, reaching deeper layers of the skin. The edema test
induced in rats showed that the nanoemulsion possessed a
strong anti-inflammatory activity when compared with the solu-
tion, reaching maximal inhibition of edema over 24 hours, as
well as not showing irritation. The researchers concluded that
the nanoemulsion was a system that met the best attributes for
transdermal application of meloxicam, with good spread ability
and an adequate liberation profile.
Good permeation and bioavailability profiles for nanoemul-
sions were also found in the study by Alvarado et al.,34 whose
objective was to propose and optimize a nanoemulsion with nat-
ural or synthetic pentacyclic triterpenes with recognized
anti-inflammatory activity.34 The results of the tests showed an
elevated capacity for permeation of the skin in ex vivo tests and
good anti-inflammatory activity with topical application, with the
developed formulation also not showing toxic or irritating effects
on the skin in in vivo tests. Another study of nanoemulsions with
a natural base sought to assess the permeation profile ex vivo
and the anti-inflammatory activity in vivo of nanoformulations
with a four-flavonoid base isolated from the leaves of Eysen-
hardtia platycarpa.35 The results of the test showed that the
nanoemulsion has a significant advantage in the improvement
of the therapeutic effect and a reduction of secondary effects,
with the consequent improvement of permeation, as well as
having adequate anti-inflammatory effects. Therefore, the stud-
ies showed the adequacy of the nanoemulsions developed in
terms of anti-inflammatory effects via topical administration and
better performance in relation to other formulations studied,
beyond having good cutaneous tolerance.33–35
Anticarcinogenic activity
It is unquestionable that cancer is a public health problem,
given that it is one of the most frequent in populations today.
Recent global estimates showed that globally in 2012, 232,000
new cases of melanoma were diagnosed, with 55,000 deaths.
In Brazil, nonmelanoma skin cancer continues to be the tumor
with highest incidence in both sexes, responsible for approxi-
mately 20% of new cancer cases.36 Given this, the develop-
ment of new medications for diverse modes of treatment has
International Journal of Dermatology 2018
6 Review Nanoemulsions and dermatological diseases
been widely studied, with the aim of reaching the target tissue
quickly and efficiently. One study assessed the properties
in vivo and in vitro of a second-generation photosensitizing drug
widely used in the treatment of skin cancer, using nanoemul-
sions as a vehicle for drug liberation.37 The tests showed that
the photosensitizing properties of the drug were maintained
after its incorporation into the nanoemulsion, but the permeation
flow was increased when compared with the physiological med-
ium, a phenomenon that resulted in greater accumulation of the
drug in the deeper skin layers and better interaction with the tar-
get tissues. Results presented the nanoemulsions as potentially
effective and promising administration systems for medications.
In addition, more recent research also evaluated the photosen-
sitizing efficacy of a new nanoemulsion containing acßaı oil to
induce melanoma cell death in in vitro and in vivo models.
The nanoemulsion was shown to kill 85% of melanoma cells,
maintaining high viability in normal cells, and treated mice
showed 82% tumor reduction compared with the control group.
These results presented the nanoemulsions as potentially effec-
tive and promising drug delivery systems.
In a xenograft model of human melanoma in rats, Tange
39
et al. compared the efficiency and safety of a nanoemulsion
and a suspension as delivery systems for Dacarbazine medica-
tion in antineoplastic treatments. The results showed that the
topical application of the nanoemulsion with Dacarbazine was
more effective in comparison with the suspension, with a reduc-
tion in tumor size up to 10 times greater percentage wise. In
addition, 12 weeks after ceasing treatment, the nanoemulsions
presented an efficacy five times greater in the prevention of
tumor recurrence in comparison with the suspension (73%
against 14%), with fewer secondary adverse effects. In another
comparative study carried out by researchers from the same
group in 2011, it was investigated if there was an increase in
the efficacy of the nanoemulsion with Dacarbazine in relation to
the suspension in the treatment of topical epidermoid carci-
noma.40 The final size of the tumor that received the nanoemul-
sion topically significantly diminished in comparison to the
suspension, generating a treatment efficacy 10 times greater. In
addition, no adverse effects such as ulcers and/or discoloration
of the skin were observed, as were with the suspension. There-
fore, it can be seen from these studies that the increased effi-
cacy and reduction of adverse effects achieved using
formulations in nanoemulsions is attributed to the reduced
dimension of the particles and the possibility of making soluble,
in a lipophilic medium, water-soluble compounds. This made
topical application an adequate means for the delivery of anti-
neoplastic agents and potentially reduced toxicity.
Another study, which sought to evaluate the toxicity and effi-
cacy of the compounds in the treatment of skin cancer, tested
the activity of daunorubicin in a cholesterol-rich nanoemulsion
on rats with melanoma, when compared with its commercial
presentation.41 The tests showed an elevated superiority of the
nanoemulsion over the commercial presentation
International Journal of Dermatology 2018
de Souza et al.
daunorubicin, both in the in vitro and in vivo tests. There was a
reduction in the growth of the tumor in 59% of rats for the treat-
ment with the nanoemulsion and increased survival rates, which
were not observed with the commercial medication. In addition,
the number of rats with metastasis was reduced from 82% to
just 30%, and the maximum dose of the drug tolerated was 65
times greater in the nanoemulsion than in the commercial
daunorubicin. Therefore, the formulation in nanoemulsion was
more stable, with improved rates of tumor growth inhibition and
of survival, with relevant lower toxicity in vivo.
Therefore, the nanoemulsions conferred on the antineoplastic
drugs an improved bioavailability and safety profile, given that the
majority of these have weak bioavailability and are associated with
an increase in secondary effects.39–41 As such, when a chemother-
38
apy agent is delivered by a vehicle such as a nanoemulsion, its
local administration achieves a uniform distribution, improves per-
meation, and, consequently, is more effective.
Final considerations
In summary, nanoemulsions were responsible for an increase in
permeation of active principles into the skin, which resulted in
improved bioavailability and efficacy of diverse compounds with
anti-inflammatory, antifungal, antimicrobial, and anticarcinogen
compounds, with a consequent therapeutic improvement for
treatment of the dermatological diseases tested. Good liberation
profiles for the drugs were obtained, which resulted in better,
more long-lasting effects, presenting superior properties in
terms of performance in comparison with conventional products.
In addition, the compounds presented adequate physical prop-
erties, which remained stable over the long term. In this way,
nanoemulsions for topical application are considered as superior
alternatives to conventional formulations of lipophilic drugs. This
assessment is based on its better permeation properties,
improved pharmacokinetic profile, and, consequently, better
therapeutic efficacy.
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International Journal of Dermatology 2018