VIETNAM NATIONAL UNIVERSITY IN HO CHI MINH CITY

SCHOOL OF MEDICINE
Department of Pharmaceutics and Biopharmaceutics

PHARMACEUTICS AND BIOPHARMACEUTICS 2

REPORT
EMULSIONS AND OINTMENTS

Topic: Identify three topical diseases where each of the four various types
of ointment bases might be employed to deliver (an) API(s). For each
specific topical affliction, identify three drugs whose topical concentration
differs that can be used for the treatment.

CLASS : D2020
GROUP :6
MEMBERS :5

No. Fullname Student ID Campus email

1 Phạm Bùi Nam Anh 207720201003 pbnanh.d2020@medvnu.edu.vn

2 Nguyễn Thành Đạt 207720201007 ntdat.d2020@medvnu.edu.vn

3 Trần Anh Đức 207720201010 taduc.d2020@medvnu.edu.vn

4 Dương Thị Mỹ Huyền 207720201016 dtmhuyen.d2020@medvnu.edu.vn

5 Hoàng Thị Ngọc Lan 207720201021 htnlan.d2020@medvnu.edu.vn

06/03/2024
Ho Chi Minh City
Table of Contents
I. INTRODUCTION..........................................................................................................1
II. OVERVIEW OF SKIN DISEASES.....................................................................................2
1. Atopic dermatitis...............................................................................................................2
1.1. Introduction..................................................................................................................................2
1.2. Causes............................................................................................................................................2
1.3. Symptoms......................................................................................................................................2
2. Acne...................................................................................................................................2
2.1. Introduction..................................................................................................................................2
2.2. Causes of Acne..............................................................................................................................2
3. Psoriasis.............................................................................................................................2
3.1. Introduction..................................................................................................................................2
3.2. Causes of Psoriasis........................................................................................................................3
3.3. Variants of psoriasis......................................................................................................................3

III. OVERVIEW OF OINTMENTS.....................................................................................3

1. Ointments..........................................................................................................................3
2. Classification......................................................................................................................3
2.1. Hydrocarbon/ oleaginous bases...................................................................................................4
2.2. Absorption bases...........................................................................................................................4
2.4. Water-soluble bases......................................................................................................................5

IV. AVAILABLE OINTMENT PREPARATION....................................................................7

1. Eczema...............................................................................................................................7
2. Acne...................................................................................................................................7
3. Psoriasis.............................................................................................................................9
V. CONCLUSION............................................................................................................11
VI. BIBLIOGRAPHY.......................................................................................................1
I. INTRODUCTION
Topical disease is one of the most common human illnesses in the world. All age
groups, especially children, and cultures are affected, and from 30% to 70% of people
are affected overall, with considerably greater proportions in at-risk groups [1].
Topical medications are being researched and used to treat these skin diseases.
Topical medication is typically applied to bodily surfaces such as the skin or mucous
membranes to treat diseases. It comes in a variety of forms, including creams, foams,
gels, lotions, and ointments [2]. In this essay, we shall discuss some topical ointments
in varying doses. In addition, we will review the benefits of these drugs for three
common skin diseases: atopic dermatitis, acne, and psoriasis.

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II. OVERVIEW OF SKIN DISEASES
1. Atopic dermatitis
1.1. Introduction
Atopic dermatitis (eczema) is a chronic, non-infectious skin condition that causes skin
irritation, redness, and inflammation. It is common condition that usually begins in
childhood [3].
1.2. Causes
There are some factors that lead to developing eczema. First is a genetic defect in the
FLG gene which encodes the production of profilaggrin (a large protein found in the
cells that make up the skin’s outermost layer) [5]. This can cause a 50% less protein
expression, which worsen the disease [4]. The second factor is family history of
allergies which present in 70% of eczema patients [4]. The third factor is the immune
system issues. Finally, environmental factors can also increase the risk of disease [5].
1.3. Symptoms
Itching is the most common symptom of eczema, and it can worsen. Additional
typical symptoms include dry, red skin areas; rashes that, when scratched, may ooze,
leak a clear liquid, or bleed; skin that gets harder and thicker. In areas of skin
inflammation, patients with darker skin tones frequently notice a darkening or
lightening of the skin.[3]
2. Acne
2.1. Introduction
Acne is a skin condition that occurs when your hair follicles become plugged with oil
and dead skin cells. Acne outbreaks occur on the face but can also appear on the back,
chest, and shoulders [6].
2.2. Causes of Acne
 Excessive or elevated oil production within the pore.
 Dead skin cell accumulation inside the pore.
 Bacterial growth within the pore [6].
The primary cause of teenage acne is the increased production of androgen hormones
during puberty [7]. Sebum protects the skin and helps it stay moisturized. However, if
a layer of dead cells blocks a pore’s opening, sebum is unable to exit. It accumulates
in the sebaceous glands causing the formation of blackheads or whiteheads. If that
area becomes inflamed, it develops into a pimple [7]. Furthermore, there are a number
of other causes of acne such as: genetic factors, age, use of certain medications
containing hormones, corticosteroids, and lithium [6].
3. Psoriasis
3.1. Introduction
Psoriasis is a chronic, common, inflammatory skin disease. Characteristics are scaly,
clearly demarcated erythematous plaques, often found on the extensor muscle surface.

3
Patients with psoriasis are highly affected by a range of systemic problems and
comorbidities that are linked to the condition [8].
3.2. Causes of Psoriasis
It is believed that psoriasis is related to immune disorders and genetic factors, and
lesions flare up when favorable factors are encountered. According to genetic factors,
psoriasis is common in people with HLA-CW6 gene which is found in 87% of the
patients [9]. Factors that can cause the disease: stress, corticosteroid use, history of
endocrine disorders, metabolic disorders or alcoholism, etc.
3.3. Variants of psoriasis

Figure 2.1. Plaque Psoriasis [8] Figure 2.2. Scalp psoriasis [8]

Figure 2.3. Pustular psoriasis [8] Figure 2.4. Nail Changes [8]

III. OVERVIEW OF OINTMENTS

1. Ointments
Ointments are semisolid preparations that incorporate a lipid or hydrophobic excipient
and are intended for external application to the skin or other muco-sal membranes
[10]. They can be medicated or not. Unmedicated ointments are used for the physical
effects they provide as protectants, emollients, or lubricants. Ointment bases, as
described, may be used for their physical effects or as vehicles for medicated
ointments. [11]
2. Classification

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Ointments are classified based on their composition and physical characteristics.
There are four general groups: hydrocarbon bases, absorption bases, emulsion or
water-removable bases, and water-soluble bases [12].

5
Table 3.1. Various types of ointment bases

2.1. Hydrocarbon/ oleaginous bases

Hydrocarbon bases are made of oleaginous materials [12]. On application to the
skin, they have an emollient effect, protect against the escape of moisture, are
effective as occlusive dressings, can remain on the skin for long periods without
drying out, and because of their immiscibility with water, are difficult to wash
off [11]. It is difficult to incorporate aqueous phases into hydrocarbon bases.
However, powders can be incorporated into these bases with the aid of liquid
petrolatum. Common hydrocarbon bases include Petrolatum, White petrolatum,
Yellow ointment, White ointment [12].
2.2. Absorption bases
Absorption bases contain an oleaginous material and a water-in-oil (w/o)
emulsifier so that they can absorb water to form or expand w/o emulsions [10].
These bases may be used as emollients and soothe the skin, although they do
not provide the degree of occlusion afforded by the oleaginous bases [11].

6
Absorption bases are of two types:
 Anhydrous bases that permit the incorporation of aqueous solutions
resulting in the formation of water-in-oil (w/o) emulsions (e.g.,
hydrophilic petrolatum) [11].
 Bases that are already w/o emulsions (emulsion bases) and permit the
incorporation of small additional quantities of aqueous solutions. For
example, lanolin and cold cream [10].
2.3. Water-removable bases
Water-removable bases are basically oil-in-water emulsions. Unlike hydrocarbon and
absorption bases, a large proportion of aqueous phase can be incorporated into these
bases with the aid of suitable emulsifying agents. It is easy to remove them from the
skin due to their hydrophilic nature. Emulsion bases include hydrophilic ointment and
vanishing cream. [12]
Table 3.2. A typical composition of hydrophilic ointment [10]

Table 3.3. A typical composition of vanishing cream [10]

2.4. Water-soluble bases

Water-soluble bases do not contain oleaginous components. They are completely
water washable and often referred to as greaseless. Because they soften greatly with
the addition of water, large amounts of aqueous solutions are not effectively
incorporated into these bases. They mostly are used for incorporation of solid

7
substances. Polyethylene glycol (PEG) ointment, NF, is the prototype example of a
water-soluble base. [11]

Table 3.4. A typical composition of water-soluble base

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IV. AVAILABLE OINTMENT PREPARATION
1. Eczema
Eczema is a long-term condition that worsens on occasion. The main symptom of this
inflammatory disease is a very itchy rash. According to the instructions from the
Ministry of Health in Vietnam, treatment principles will include:
 Use anti-dry skin and skin-soothing medicine
 Anti-infection
 Anti-inflammatory
Treatment of eczema is most effective when addressing the underlying
pathophysiologic processes. Typical treatment is the most optimal method, children
need to be bathed daily in warm water along with low alkaline soap. After that, use
skin moisturizer to prevent their skin from being dry [9]. Additionally, the support of
drugs will help ameliorate the condition and limit inflammatory flare-ups. Patients are
prescribed a variety of drugs based on the severity of the disease including
corticosteroids, antibiotic ointments, and immunosuppressants. However, topical
corticosteroids, particularly hydrocortisone, are considered the most common method
of treating eczema.
Table 4.1. Comparison of three different hydrocortisone concentration
Concentration Dosage form Ingredients

Hydrocortisone 0.5% Active: Hydrocortisone (0.5g/100g)

Inactive: White soft paraffin, Liquid paraffin [13]

Hydrocortisone 1% Active: Hydrocortisone acetate (1g/100g)

Ointment Inactive: White petrolatum, Sorbitan sesquioleate,
Mineral oil [14]

Hydrocortisone 2.5% Active: Hydrocortisone (25mg/1g)

Inactive: White petrolatum, Mineral oil [15]

Hydrocortisones 1% and 2.5% are two common types of absorption base ointment due
to its occlusion and lubrication which increases steroid absorption [16]. In terms of
ingredients comparison between these two products, they all have white petrolatum as
a skin protectant and mineral oil as a blocker that prevents trans-epidermal water loss
to trap water in the skin [17]. However, hydrocortisone 1% also includes sorbitan
sesquioleate (SSO) which acts as a surfactant and a emulsifier and functions as a skin
soother and moisturizer [18]. In contrast, due to hydrocortisone 0.5% ointments are
not available on the market today and most are cream preparation, it is difficult to find
information about their formulations.
2. Acne

9
Numerous pharmacological agents, such as Benzoyl Peroxide, Salicylic Acid,
Retinoid, Azelaic Acid, and antibiotics are used to treat acne, particularly acne
vulgaris [19]. But we will focus on products that contain Benzoyl peroxide (BPO) – a
pharmacological agent that is frequently used to treat acne.
BPO is typically formulated in three main concentrations: 2.5%, 5%, and 10%, with
the most common formulation being in the form of gel. Gel is a kind of ointment
composed of liquid substances that the right gel-forming agents solidify [20]. With its
excellent absorption, oil control, ease of use, and less greasy feeling, gel formulations are
widely used in acne treatment.
Table 4.2. Comparison of three different BPO concentration
Commercial Concentratio Dosage Ingredients
products n form
Perrigo benzoyl 2.5% Active: Benzoyl peroxide 2.5%
peroxide gel Inactive: Carbomer homopolymer,
dimethicone, disodium lauryl
sulfosuccinate, edetate disodium, glycerin,
methyl paraben, poloxamer 182, purified
water, silicon dioxide, sodium hydroxide
[21]
Clindamycin 1%/5% Active: Clindamycin phosphate 1% and
Gel –
and Benzoyl Benzoyl Peroxide 5%.
Aqueous
peroxide gel Inactive: Carbomer homopolymer,
base
docusate sodium, edetate disodium, sodium
hydroxide, purified water [22]
Benzac Ac 10% Active: Benzoyl peroxide 10%.
treatment gel Inactive: Docusate sodium, disodium
edetate, poloxamer 182, carbomer 940,
propylene glycol, acrylates copolymer,
glycerol (glycerin), silicon dioxide, sodium
hydroxide, and purified water [23]

The main difference between these concentrations lies in the potency of the active
ingredient and the potential for skin irritation.
Effectiveness in acne treatment: A 2.5% concentration can be equally effective
compared to higher concentrations such as 5% or 10% [24].
Likelihood of irritation: Higher concentrations tend to irritate the skin more, resulting
in symptoms such as dryness, redness, peeling, and itching [24].
Furthermore, when comparing the excipients present in the three aforementioned
products, similarities can be observed in the selection of primarily used excipients to
formulate the gel dosage form:
 Carbomer homopolymer and carbomer 940: They provide viscosity and
thickening to the product by their ability to swell in water and form a gel.

10
  Disodium EDTA: A chelating agent used to sequester metal ions and
enhance product stability.
 Sodium hydroxide: Adjusts the pH of the product, ensuring stability and
skin safety.
 Purified water: The main component to formulate the liquid portion of the
gel.
 Glycerin: A moisturizing excipient.
 Poloxamer 182: Surfactants non-ionic.
 Docusate sodium: A molecule softener which has the ability to dissolve fat
molecules, making the product easier to use and absorb. [25]
Besides, products from Perrigo and Benzac Ac use other excipients to increase the
stability and quality of the product:
 Preservative excipient: Methyl paraben
 Other moisturizing excipients: Dimethicone, Propylene glycol.
 Other gel viscosity agents: Silicon dioxide, Acrylates copolymer.
As a result, all three products above have mostly the same gel preparation methods. In
the product Clindamycin and Benzoyl Peroxide gel 1%/5%, the most basic
formulation has the cheapest price, but in the remaining 2 products, there are a number
of other excipients that will help the product achieve quality and stability, better
determination.
3. Psoriasis
The treatment methods for psoriasis are diverse, with the most common being topical
treatments such as corticosteroids, vitamin D3 analogues, tazarotene, roflumilast,
tapinarof, emollients, salicylic acid, among others [26]. We will explore three
products containing Salicylic acid in various concentrations suitable for different types
of psoriasis conditions.
Salicylic acid is a keratolytic agent that helps soften scales, facilitating their removal,
and enhances the absorption of other active ingredients [26]. Salicylic acid
formulations are typically available in ointment and cream. Ointment products have
good skin penetration capabilities, providing favorable conditions for salicylic acid to
work effectively. It is also diluted in ointment formulations to create products with
appropriate concentrations and ease of application on the skin.

11
Table 4.3. Comparison of three different Salicylic acid concentration
Commercial Concentration Dosage Ingredients
products form
Salicylic acid 2% Ointment Active: Salicylic Acid 2%
ointment Inactive: wool alcohol, hard paraffin,
liquid paraffin, white petroleum jelly.
[27]
Lotusalic 3% Active: Betamethason dipropionat
ointment 0.064g, Acid salicylic 3g. [28]
Inactive: Paraffin solidum, Vaseline
e.q 100g. [28]
Salicylic acid 5% Active: Salicylic Acid 5%
5% (0.75g/15g)
Inactive: Propylen glycol, Cremophor
A6, Cremophor A25, Acid stearic,
Vaseline. [29]

Salicylic acid can be used in various concentrations ranging from 2% to 6% or more,

[30] depending on the severity of the condition. Products with lower concentrations
(1-2%), are often used for mild cases and sensitive skin. Severe skin conditions may
require higher concentrations (5-10%) which can cause toxicity and skin irritation
[30].
Furthermore, when comparing the excipients used in ointment formulation, the
majority of them are oil-based. Oil-based excipients have high stability, excellent skin
penetration, and can effectively incorporate stable API [31][32]. However, they may
feel greasy on the skin, hinder physiological skin functions, and are susceptible to
oxidation and degradation under light or heat exposure [31][32].
 Hydrocarbons such as Hard Paraffin, Liquid Paraffin, Vaseline, and White
Petroleum are characterized by their stability, resistance to degradation,
inert chemical properties, and cost-effectiveness. [31][32] They serve to
structure the product, provide softness, and retain moisture for the skin.
 Wax: Wool Alcohol (Lanolin alcohol), a natural oil substance found in
sheep's wool. Lanolin is gentle on the skin, highly absorbent, and has a
strong affinity for water and polar liquids, forming non-distinct emulsions.
[32]
 Fatty acid: Stearic Acid is used to improve the viscosity and cohesion of the
product.
 Fatty acid derivatives: Cremophor A6 and Cremophor A25 are emulsion-
forming groups that aid in dissolving water-insoluble substances into oil.

12
All three products containing salicylic acid in ointment formulations utilize commonly
found oil-based excipients, which are readily available and cost-effective.
Additionally, these excipients are suitable for providing moisture, softening the skin,
and protecting against dry and sensitive skin conditions, specifically those afflicted
with psoriasis.

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V. CONCLUSION
In summarize, all three topical diseases share basic similarities in the use of excipients
required to create the ointment dosage form, including different API concentrations.
There may also be minor differences in formulation between products, which can be
explained by two factors. For starters, commercialization creates different brands,
making the product better and more suitable for the target audience, as well as
differences in the concentration of the main active ingredient; higher concentrations
cause irritation. Therefore, some additional excipients are required to protect and
moisturize the skin.

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VI. BIBLIOGRAPHY
[1] Hay RJ, Johns NE, Williams HC, Bolliger IW, Dellavalle RP, Margolis DJ, et al.
The global burden of skin disease in 2010: An analysis of the prevalence and impact
of skin conditions. Journal of Investigative Dermatology. 2014 Jun;134(6):1527–34.
doi:10.1038/jid.2013.446
[2] Using medication: Topical medications [Internet]. U.S. National Library of
Medicine; 2017 [cited 2024 Mar 6]. Available from:
https://www.ncbi.nlm.nih.gov/books/NBK361003/
[3] Atopic dermatitis [Internet]. U.S. Department of Health and Human Services; 2023
[cited 2024 Mar 6]. Available from: https://www.niams.nih.gov/health-topics/atopic-
dermatitis
[4] Avena-Woods, C. (2017). Overview of atopic dermatitis. The American journal of
managed care, 23(8 Suppl), S115-S123.
[5] Flg Gene: Medlineplus genetics [Internet]. U.S. National Library of Medicine;
[cited 2024 Mar 6]. Available from: https://medlineplus.gov/genetics/gene/flg/
[6] Acne [Internet]. U.S. Department of Health and Human Services; 2023 [cited 2024
Mar 6]. Available from: https://www.niams.nih.gov/health-topics/acne
[7] InformedHealth.org [Internet]. Cologne, Germany: Institute for Quality and
Efficiency in Health Care (IQWiG); 2006-. Acne: Overview. 2013 Jan 16 [Updated
2019 Sep 26]. Available from: https://www.ncbi.nlm.nih.gov/books/NBK279211/
[8] Kimmel, G. W., & Lebwohl, M. (2018). Psoriasis: overview and diagnosis.
Evidence-Based Psoriasis: Diagnosis and Treatment, 1-16.
[9] Bộ Y tế, Quyết định số 75/QĐ-BYT, Hướng dẫn chẩn đoán và điều trị các bệnh
da liễu, 2015
[10] Ointments and types of ointment bases - pharmaceutical [Internet]. [cited 2024
Mar 6]. Available from: https://www.pharmacy180.com/article/ointments-and-types-
of-ointment-bases-2856/
[11] Loyd V. Allen, Jr, PhD, & Howard C. Ansel, PhD (2014). Ansel's
Pharmaceutical Dosage Forms and Drug Delivery Systems, 10th Edition.
[12] Gad, S. C. (Ed.). (2008). Pharmaceutical manufacturing handbook: production
and processes (Vol. 5). John Wiley & Sons.
[13] Electronic medicines compendium [Internet]. [cited 2024 Mar 6]. Available from:
https://www.medicines.org.uk/emc
[14] Hydrocortisone Ointment, USP 1% [Internet]. National Institutes of Health;
[cited 2024 Mar 6]. Available from:
https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=d6523993-d781-
cdbc-e053-2a95a90af191&type=display
[15] Hydrocortisone Cream USP, 2.5% hydrocortisone ointment USP, 2.5% [Internet].
National Institutes of Health; [cited 2024 Mar 6]. Available from:
https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=7ba59aa6-b828-
4048-bf86-90c90d9894a0&type=display
[16] Abimbola Farinde P. Topical corticosteroids [Internet]. Medscape; 2024 [cited
2024 Mar 6]. Available from: https://emedicine.medscape.com/article/2172256-
overview?form=fpf
[17] Bao, Q., Morales-Acosta, M. D., & Burgess, D. J. (2020). Physicochemical
attributes of white petrolatum from various sources used for ophthalmic ointment
formulations. International Journal of Pharmaceutics, 583, 119381.
[18] Mineral oil [Internet]. [cited 2024 Mar 6]. Available from:
https://go.drugbank.com/drugs/DB11057
[19] [Internet]. [cited 2024 Mar 6]. Available from:
https://www.benhvien108.vn/duoc-lam-sang/thuoc-dieu-tri-mun-trung-ca.htm
[20] Lê, Q. N., Huỳnh, V. H., & Lê, V. L. (2007). Bào chế và sinh dược học: tập 2:
dùng cho đào tạo dược sĩ đại học: Mã số Đ. 20. Z. 04: tái bản lần thứ 1.
[21] DailyMed [Internet]. National Institutes of Health; [cited 2024 Mar 6]. Available
from: https://dailymed.nlm.nih.gov/
[22] Commissioner O of the. MedWatch: FDA Safety Information & Adverse Event
Reporting Program [Internet]. FDA; [cited 2024 Mar 6]. Available from:
https://www.fda.gov/safety/medwatch-fda-safety-information-and-adverse-event-
reporting-program
[23] Benzac AC treatment gel 10% [Internet]. [cited 2024 Mar 6]. Available from:
https://www.benzac.com/nz/product/benzac-ac-treatment-gel-10
[24] Mills Jr, O. H., Kligman, A. M., Pochi, P., & Comite, H. (1986). Comparing
2.5%, 5%, and 10% benzoyl peroxide on inflammatory acne vulgaris. International
journal of dermatology, 25(10), 664-667.
[25] National Center for Biotechnology Information (2024). PubChem Compound
Summary for CID 23673837, Docusate Sodium. Retrieved March 6, 2024 from
https://pubchem.ncbi.nlm.nih.gov/compound/Docusate-Sodium.
[26] Das S. Psoriasis [Internet]. MSD Manual; 2024 [cited 2024 Mar 6]. Available
from: https://www.msdmanuals.com/professional/dermatologic-disorders/psoriasis-
and-scaling-diseases/psoriasis
[27] Electronic medicines compendium [Internet]. [cited 2024 Mar 6]. Available from:
https://www.medicines.org.uk/emc
[28] [Internet]. [cited 2024 Mar 6]. Available from:
https://www.nhathuocankhang.com/thuoc-tri-benh-da-lieu/lotusalic-15g
[29] [Internet]. [cited 2024 Mar 6]. Available from:
https://nhathuoclongchau.com.vn/thuoc/salicylic-5-hataphar-hop-tuyt-15g-31994.html
[30] Torsekar, R., & Gautam, M. M. (2017). Topical therapies in psoriasis. Indian
dermatology online journal, 8(4), 235.
[31] [Internet]. [cited 2024 Mar 6]. Available from: https://trungtamthuoc.com/bai-
viet/thuoc-mo-la-gi-uu-nhuoc-diem-va-phuong-phap-bao-che-thuoc-mo
[32] Võ, X. M., Nguyễn, V. L., & Phạm, N. B. (2004). Kỹ thuật bào chế và sinh dược
học các loại thuốc: tái bản lần thứ nhất: tập 2.