Novel Drug Delivery Systems of Herbal Constituents Used in Acne

 

Surekha Baghel, Bina Gidwani, Chanchal Deep Kaur*

Shri Rawatpura Sarkar Institute of Pharmacy, Kumhari, Durg (C.G.)

*Corresponding Author E-mail:

 

ABSTRACT:

Novel technologies have been developed advanced research for drug delivery systems. Plant based medicines are used from ancient time for treatment of diseases. Drug delivery system is very important to decide the administration of drug, to overcome the disadvantages of traditional or other delivery system. The main goal for making the herbal NDDS system is to minimize the drug degradation taken by oral route of drug and   harmful side effects and increases the bioavailability. The herbal NDDS delivery system is to make the drug control release as well as sustain drug action, at a predetermined rate, to maintain a relatively constant, effective drug level in the body with minimization of undesirable side effects. The main reason behind for the formulation of NDDS is to make sustain and control release of drug for better therapeutic effect. The method by which a drug is delivered can have a significant effect on its efficacy. Some drugs have an optimum concentration range within which maximum benefit is derived, and concentrations above or below this range can be toxic or produce no therapeutic benefit at herbal novel drug delivery system is better than synthetic NDDS .Because of their less toxicity and better therapeutic action. In NDDS we knows its predetermination release rate, thus it reduces toxicity by decreasing the dose frequency. Now a day’s liposome, ethosome, phytosomes, emulsions, microsphere, solid lipid nanoparticles, niosomes, hydrogel of herbal formulation has enhanced the therapeutic effects of plant extracts.

 

KEYWORDS: Plant constituents, skin disorder, NDDS, toxicity.

 

 


1. INTRODUCTION:

Skin is the largest organ which covers the whole body. It is the outer most layers which we called as integumentary system. Skin is composed of three different layer epidermis, dermis and hypodermis.  Skin is composed  main function of skin is to protect body against pathogen, excessive water loss, temperature regulation, synthesis of vitamin D. skin diseases cause due to imbalance in perspiration of skin cell with the environment. The sweat containing urea is excreted to skin which is responsible for body temperature.

Skin diseases are classified in to two classes which are following as:

a) Acute skin diseases: this can be cure in easily and can’t show patches or marks after treatment. 

b) Chronic skin diseases: this can take long term treatment for cure.

 

Some of the common skin diseases are:

 

Table1. List of some common skin diseases

S. no.

Common skin diseases

Details

1.

Eczema

It is types of skin disease in which causes the skin become inflammated or infected.

2.

Psoriasis

 These are a type of disorder produces thick plaques covered with silvery scales.

3.

Rosacea

It causes redness on nose, chin, cheeks, and forehead.

4.

Ichy skin  or rashes

these cause irritation, allergy, infections which is followed by area of redness and inflammation

5.

Trauma

It is a type of injury to skin caused by cut, burn or inflammed body surface

6.

Acne

In this type of diseases inflammation of the skin, due to blockage of your skin’s pores.

7.

Sunburn

In this type of diseases outer layer of skin burn with direct contact of sun rays

8.

Cellulite

Cellulite is normal fat beneath the skin. The fat appears bumpy because it pushes against the connective tissue beneath the skin, causing the skin above it

to pucker

9.

Blister

Blisters occur in all size. This bisters are some painful, red,or itchy and other aren’t .

.

 

 

1.1   Current scenario of skin diseases

In the above (table.1) we had studied that some common skin diseases but as per current scenario we had studied that acne is the most common skin diseases around 80% of person affecting between 11 to 30 years old at some point. About 4.8 million patient per year affected with acne. It can persist for  years resulting it causes  disfigurement of face skin ,also it showed not clear, permanent scarring, emotional problem like depression related to their skin diseases.  So our main focus to studied about acne skin disease and give some information to relief those patient how suffering from this type of diseases.

 

1.2 What is Acne ?

Acne is a skin disease which is commonly known as pimples.  Pimple is type of acne. Acne can occur more in oily skin type because they can secrete more amount of sebum which is responsible to block the follicles leads to skin diseases. Acne occurs in mostly in teenagers [1]. Through literature survey we studied that males are more affect by acne as compare to females. It is types of chronic disorder of placebo unit.

 

 

According to W.H.O “Acne is an inflammatory disease of the pilosebaceous units in the skin of the face, neck, chest and upper back”. Acne initially appears during when the onset of puberty at the time when triggers androgenic stimulation it produce excessive level of sebum and abnormal follicular keratin and it occurs due to presence of Gram-positive bacterium (Propionibacterium acnes) and causes local inflammation. P. acne produces inflammation because of through the production of extracellular products such as lipases, proteases, hyaluronidases and chemotactic factors.

 

1.2.1 Types of acne

Acne is an inflammantory skin disease on the basis of inflammation is classified in three ways which are following as:

 

Mild acne: Mild acne includes two type white heads and blackheads. Whiteheads means clogged pores are closed with skin surface. Blackheads means clogged pores are opened at the skin surface and it easily more noticeable and visible in skin.

 

Moderate acne: It is such severe inflammatory acne which also includes whiteheads and blackheads plus papules. Whiteheads plus papules in which some areas reddened that are elevated above the skin and in blackheads plus papules small bumps on the skin that contain fluid which are easily.

 

Nodulocystic acne: In this type of acne nodules are produced in deeply embedded solid, often painful lesions. It also causes some additional infections. Nodules size can be greater than 5mm in diameter.[1]

 

1.2.2Causes of acne

The exact causes of acne are unknown. There are some factors which play main role for risk the acne which are following as:

1)   Age:  Hormonal changes occur due to age experience, more acne develop in teenagers.

2)   Gender: as compare to girls boys had more severe acne.

3)   Disease: mainly complicate acne in girls due to hormonal disorders.

4)   Heredity: It also occurs due to family history of acne have greater chances susceptibility to the disease.

5)   Hormonal changes: acne can come out before menstruation, during pregnancy and menopause.

6)   Diet: Some foods cause acne like fatty diet , irregular diet it also cause acne.

7)   Drugs : Such drugs like tranquilizers, antidepressants, antibiotics, oral contraceptives and anabolic steroids  can cause acne due to their side effect

8)   Environment: It also occurs due to exposure of oils and greases, polluted air and sweating in summer it aggravate acne.

9)   Stress: Emotional stress , depression also may be contribute for acne.

 

1.2.3 Treatment of acne by allopathic drugs

The main mechanism to treatment of acne is altering the pattern of follicular keratinisation, decreasing activity of sebaceous gland, also decreasing population of P.acneand producing anti-inflammatory effects.For treatment of mild acne some drug Benzoyl peroxide works to reduce oil made by the glands.  Resorcinol, salicylic acid, and sulphur help breakdown whiteheads and blackheads. Such broad spectrum antibiotics such as erythromycin, clindamycin (Cleocin-T), and meclocycline (Meclan); also used to cure acne.Other treatments for acne available which is surgical or medical treatment such as: Comedone extraction, Chemical peels , Punch grafting, Intralesional injection and Collagen injection. Now a day’s researcher  develop therapeutic modalities and various formulation and combination had been designed in topical agent (benzoyl peroxide, retinoids, antibiotics etc.)but their combination causes some side effect when tried on patients that increase the frequency and severity of dryness, scaling , erythema, burning , stinging and itching[3]. Minocycline had a severe risk of adverse of side effects as compare to other tetracycline. It may also induce hypersensitivity(it affecting liver, kidney or lungs ) , long term treatment of acne may cause autoimmune disorder. On other hand, some CNS symptoms occur such as dizziness is more frequent as compared to other tetracycline. Long term treatment may also cause hyper-pigmentation of the skin [4]. Treatment with chemotherapy generally lasts from several weeks to months but it may be extended for long period of time. When oral antibiotics used for long term it creates tremendous selective pressures for the higher resistant strains of   P. acnes.


 

 

1.2.4. Phytoconstitents used in treatment of Acne:

S.

NO

NAME OF PLANT

BIOLOGICAL SOURCE

FAMILY

CHEMICAL CONSTITUENT

USES

PART USED

REF.

1

Amarantha

Amaranthus Hypochondriacuslinn

Amaranthaceae

Saponin

Astringent, Eczema

Seed

10

2

Arnica

Arnica Mountanalinn

Asteraceace

Helenalin Dihydrohelenaline esters

Antioedema

Antimicrobial

Antiinflmatory

 

Flowers

10

3

Asparagus

Asparagus officinalislinn

Liliaceae

Aspergioloside (A to I) , asparagusic acid

Cleanging the face.

Root and rhizome

10

4

Brich

Betulaalbalinn

Betulaceae

Guaiacol, Salicylic acid, Terpenoid

Cosmetics and diuretics(w)

Barks and leaves

10

5

Burdock

Arctiumlappalinn

Asteraceae

Arctiopicrim(Sesquiterpenes), arctigenin lactose(liganan)

Antifungal

Antimicrobial

Root, seed and leaves

9

6

Barberry

(Alkaloids)

Berberis vulgaris

Barberine

 Berberine, berbamine and palmatine.

Antiandrogenic, antiinflamatory, antbacterial

Root and bark

9

7

Basil

Ocimumbasilicum and sanctum

Laminaceae

Methyl cinnamaldehyde

Antiinflamatory, antibacterial, antioxidant and antifungal

Leaves

 

9

8

Calendula

Calendula Officinalislinn

Asteraceace

Terpenoids, flavanoids (Querecetin) saponin (Arvenoside A)

Triterpinoids

Antioxidant, anti-inflamatory, antibacterial and antiviral activities

Flowers

9

9

Celandine

Chelidoniummajuslinn

 

Papaveraceae

Isoquinoline Alkaloids of Proberberine, Benzophenatherene and Protopine type

Analgesic, antisplasmodicandantiinflamatory

Parts of plant above ground and roots

10

10

Chaste tree(Vitex)

Vitexangnus Castuslinn

Verbenaceae

Viticinditerpene, rotufuranviterxilactone Flavonoid Casticin

Menstrual irregularities, skin reaction

 Fruit

10

11

Cinnamon

Cinnamomumzeylanicum

Lauraceae

Cinnamaldehyde

Antibacterial

Bark

10

12

Coriander

Coriandrum Sativumlinn

Apiaceae

Linalool, P-cymene, Geraniol, hydroxycoumarins

 

Antifungal

Antibacterial

Leaves

10

13

Guggul

Commiphoramukul

 Burseraceae

Guggulsterone

anti-inflammatory and antibacterial

Gum

9

14

Ginger

Zingiber officinale

Zingeberaceace

6-Gingerol

Antimicrobial, antiseptic, antifungal, antiinflamatory

Rhizomes

9

15

Garlic

Allium sativum

Amaryllidedaceae

Selenium, arginin

Antifungal and antibacterial

Bulb

9 and 10

16

Jojoba oil

Simmondsiachinensis

Buxaceae

Monoester of C-20 and C-22

Antibacterial, antioxidant

Leaves

10

17

Labraor tea

LedumGroenlandicumoedess

Ericaceae

Tannic acid, arbutin, ledol, Plaustrol

Astingent

Skin alinment

Leaves

10

18

Lavender

L.angustifolia mill

Lamiaceae

Linaloyl acetate, Caryophyllene oxide, cineole, linalool

Anti-inflammatory

Antibacterial

Flower

9

19

Lemon

Citrus limonlinn

Rutaceace

Gentisic acid, Hesperidin, eriocitin.

cleaning agent

Lemon juice

10

20

Licorice

Glycyrrhizaglabra

Fabaceae

glycyrrhetinic acid

Anti inflammatory,

antibacterialand soothing properties

Root

9

21

Mint

Calaminthagraveolens

Lamiaceae

Menthone, mentylcetatementhone

Antibacterial and soothing, sedative effects

Leaves

9

22

Neem

Azardiractaindica

Meliaceae

Triterpinoids and tetranortriterpene

Antibacterial, antifungal

Leaves

10

23

Orange peel

Citrus aurantiumlinn

Rutaceae

Linolyl acetate Geraniol, limonene

Antioxidant

Peel

10

24

Pine

Pinus

Pinaceae

Itmonline

Antiagenging

Bark

10

25

Rhubarb

Rheum officinaleBaill

Polygonaceace

Anthraquinone ( rhein, emodin, chrsophanol)

Relif itching and pain in Psoriasis

Rhizome

10

26

Rose

Rosa speciesb

Rosaceae

SeugeninPentogalloyl, PyrogallolMonoterpenoids, 

Antibacterial anti-inflammatory

Flowers

10

27

Soap wort

Saponariaofficinalislinn

Caryophyllaceae

Saponin D

Surface active agent ss(Cleansing)

Flowers

10

28

Tea tree oil

Melaleucaalternifolia

Myrtaceae

Terpin-4-ol

Antibacterial

Leaves

9 and 10

29

Thyme

Thymus linn

Luminaceae

Carvacrol,

P-cymene, Thymol acetate

Antibacterial

Leaves

10

30

Turmeric

Curcuma longa

Zingiberaceae

Turmerol, curcumins

Antioxidant, wound healing,

antiinflammatory

Rhizome

9 and 10

 

 

1.2.5 Following are the drugs having anti-acne activity:

 

 


1.2.6 Novel drug delivery system:

The main reason behind the formulation of NDDS is to make sustain and control release of drug for better therapeutic effect. The novel drug delivery is better than synthetic NDDs because their toxicity is less. Now days the NDDS formulation shows tremendous growth in field of skin diseases. Disadvantage of herbal NDDS it is costly as compare to other delivery system. Only reason for use of NDDS that it goes exactly at the site of action and gives the better result. Advantage is that it releases the toxic effect, decreasing the dose frequency.

 

Resent development in NDDS delivery of Herbals is:

1)   Liposomes

Liposomes are novel drug delivery  system, which are micros opical vesicles  size (0.05- 5.0µm) in a diameter  which is consisting of a diameter , which is consisting of an aqueous core enclosed in one or more nature synthetic phopholipid(4). The liposomes are mostly spherical shaped particles that encapsulate the solvents which are free floating in the interior parts of delivery system. Mostly liposomes are used to deliver such type of various type of vaccine, drugs, enzymes or other substances to target organs or cell.

 

Advantages:

     i.        The drug delivery of drug in both hydrophilic as well in hydrophobic.

    ii.        There is a possible for making both sustain and controlled release formulation.

  iii.        It increases efficiency, stability and therapeutics index.

  iv.        It improved the pharmacokinetic effect by reduce elimination increase circulation

    v.        They are highly biocompatible in delivery of drug.

 

2)   Niosomes

Nanotechnologyis a science which deals with the particles of nanorange (1-109 nm).  The niosomes are made up of non ionic surfactant with the unilaminar vesicles ad multilayer vesicles. The main difference between liposomes and niosomesor we say the main advantage is the chemical differences in to monomer unit.

 

Advantages:

     i.        They are cheaper as compare to liposomes

    ii.        They are non ionic in nature and there less toxicity.

  iii.        The functional group attached on the surface their hydrophilic head.

  iv.        They are biodegradable and non immunogenic in nature.

    v.        They are chemically stable and have long storage time capacity as compare to liposomes.

 

3)           Phytosomes :

They are complex molecular structure made up of lipid. Phyto means plant and some means cell like structure. The phytoconstituents of herbs are enclosed in a vesicular drug delivery in which the lipid is bonded to it. Some of the flavanoids, gylcosides and terpenoids  are water soluble which show less absorption.

 

Advantages:

     i.        It enhances the bioavailability

    ii.        They bonds formed between phosphatidyl choline molecule and pytoconstituent shows better stability and have high entrapment efficiency.

  iii.        It enhanced permeation of drug through skin, so used in trandermal drug delivery.

  iv.        They are used in pharmaceutical and cosmetic preparation because they are safe.

    v.        They are so effective that a small quantity will achieve the desired effect.

4)   Ethosomes

They are made up of lipid vesicles containing both lipid and alcohol, mainly ethanol and isopropyl alcohol are commonly used. Ethosomes contain high concentration of ethanol, due to which they are more stable, and used also as topical drug delivery. Ethosomes reaches to deeper skin layer due to its high concentration and permeability.

 

Advantage

     i.        Enhanced permeation of drug through skin leads to topical application.

    ii.        They are safe so used in pharmaceutical and cosmetic preparations.

  iii.        Ethosome are used in wide range of drug delivery.

  iv.        They are semisolids like gel and cream which covers wide range of drugs.

    v.        They have so many applications such as cosmetics, transdermal delivery of hormones, as a drug carrier etc.

 

5)   Transferosomes

The term transferosomes was coined by Gregorcevk in 1991. It made up of two word “transfere” and “soma”, transfere is a Latin word which means caring across and soma is a Greek word means body. They act as potential carrier for transdermal drug delivery. To overcome the difficulty related to penetration in skin tansferosomes are made.

 

Advantage

     i.        They are highly lipophilic drug nearly 90%, which shows high entrapment efficiency.

    ii.        Transferosomes are used in systemic and topical delivery of drugs.

  iii.        They are made up of natural phospholipids which are biocompatible and biodegradable.

  iv.        Transferosomes are used in delivery of corticosteroids through skin.

    v.        High trapping efficiency due to hydration from organic solvents.

 

CONCLUSION:

The main aim of selecting the herbal drugs safe and effective. Due to their quality the herbal drug is accepted all over the world. Novel drug delivery system of herbal medicine is to make drug sustain and controlled release formulation which high effectiveness and enhance bioavailability. Hence we all suggested promoting the use of herbal drugs.

 

ACKNOWLEDGMENT:

The authors are thankful to the Principal and Management of Shri Rawatpura Sarkar Institute of Pharmacy for providing necessary facility for this work. The authors are also thankful to CGCOST/ MRP/1106/2015 for providing financial assistance related to this work.

 

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Received on 11.04.2017       Accepted on 28.05.2017     

© Asian Pharma Press All Right Reserved

Asian J. Res. Pharm. Sci. 2017; 7(2): 57-67.

DOI:  10.5958/2231-5659.2017.00009.1