A REVIEW ON ENHANCING THE BIOAVAILABILTY OF …

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Shukla et al. World Journal of Pharmacy and Pharmaceutical Sciences

A REVIEW ON ENHANCING THE BIOAVAILABILTY OF

GRISEOFULVIN BY SOLID DISPERSION LOADED GEL

Sonam Shukla*, Rajneesh Kumar Gupta, Swarnakshi Upadhyay and Prateek Kumar

Kanpur Institute of Technology & Pharmacy, Kanpur.

ABSTRACT

Out of many, one of the most promising strategies to improve the oral

bioavailability of grisofelvin drugs is to develop amorphous solid

dispersions. Reduction in drug particle size improves drug wettability

and oral bioavailability significantly. Poorly soluble drugs are

benefited by formulation approaches that overcome the issue of poor

solubility and dissolution rate limited bio availability. Hence, to

improve the solubility and dissolution of grisofelvin drugs, several

formulation approaches can be considered, among which formulating

the active pharmaceutical ingredient (API) in an amorphous form is

recently gaining prominence. Formulating amorphous solid dispersions of grisofelvin drugs

with water-soluble carriers has reduced the incidence of these problems and enhanced the rate

of dissolution. This review mainly focuses on advantages, classification of solid dispersion,

methods of preparation, and characterization of the amorphous solid dispersion.

KEYWORDS: Griseuofelvin, Solid dispersion loaded gel, Bioavialbilty, Povidone,

Mannitol.

INTRODUCTION

Today around 35- 40 percent of the drug coming from high-throughput screening are poorly

soluble in water.[1]

It is well known that drug efficacy can be severely limited by poor aqueous

solubility. The ability to increase aqueous solubility is thus a valuable aid to increase the

efficacy of certain drugs.

Among the various parameters those hinder the development of pharmaceutical products and

restrict the bioavailability of oral products solubility is the most important to be deemed for

formulation scientist.

WORLD JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES

SJIF Impact Factor 7.632

Volume 10, Issue 9, 1142-1155 Review Article ISSN 2278 – 4357

*Corresponding Author

Sonam Shukla

Kanpur Institute of

Technology & Pharmacy,

Kanpur.

Article Received on

29 June 2021,

Revised on 19 July 2021,

Accepted on 09 August 2021

DOI: 10.20959/wjpps20219-19852


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In therapeutic application, continuous infusion by intravenous route is considered to be the

most superior way to administer drug in order to maintain constant drug level in plasma as well

as to bypass the first pass metabolism in liver. This infusion though is associated with risks like

phlebitis, extravasation/infiltration, air embolism, hypervolaemia and infection.

The topical route has been used over years for delivering drugs at the point of immediate action

and hence it is well known that sufficient quantity of drug is infused into the systemic

circulation so as to provide the desired therapeutic effects.

Over the recent times, almost all benefits of the intravenous infusion have had been duplicated

with lower risks utilizing skin as the doorway for administration of drugs. The skin has been

found to have continuous drug infusion into systemic circulation.

Skin – The biological barrier

Skin, the largest organ in the human body, serves as a physical barrier between the body and

the surrounding environment. It also poses as a first line of defense against pathogens, prevents

loss of water and impedes the entry of chemicals by functioning as a barrier. The two main

structural layers of the skin are the epidermis and dermis. The epidermis consists of five strata:

corneum, lucidum, granulosum, spinosum and basale. The dermis consists of layers of

collagen fibers, elastic fibers, blood and lymph vessels, soft connective tissue and nerve

endings. The barrier function of the skin is primarily provided by the stratum corneum (SC) of

the epidermis. Keratinocytes originating in the basal layer of epidermis migrate to the stratum

granulosum (SG) and are transformed into corneocytes by the process of cornification

(programmed cell death) resulting in formation of tight brick like structures with the

intercellular spaced filled with lipids thus presenting tight barrier like structure.

As passive diffusion remains the prime transport pathway across the skin, the physicochemical

characters of the penetrant as well as the delivery system and pathological state of the skin

remain the most important factors that influence the transdermal permeability of drugs.

Emulsions, both oil-in-water (O/W) and water-in-oil (W/O) type, have long been used as

topical drug delivery systems for different molecules. However, the inherent thermodynamic

instability and limited drug loading capacity are two main challenges with emulsions as drug-

delivery system.


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Drug penetration across skin

Drugs applied onto the skin can enter through different routes of penetration. Drugs enter either

via SC (transepidermal route) or the appendages (transappendageal route). The

transappendageal route, also called the shunt route, as it circumvents the SC cells, consists of

a drug transport via the eccrine glands and pilosebaceous unit (i.e., hair follicles with their

associated sebaceous glands).

The transepidermal route through the SC consists of two pathways: intercellular and

intracellular. The intercellular pathway consists of lipids, which are rich in ceramides, free

sterols, free fatty acids, along with low quantities of glycolipids, sterol esters, triglycerides,

cholesterol sulfate and hydrocarbons.The intracellular pathway, consisting of corneocytes

bound by lipoidal envelope, is utilized by hydrophilic drugs. However, it is imperative for

hydrophilic molecules to cross the intercellular lipid matrix to enter the corneocytes. The

bilayer structure, which is believed to be impervious to hydrophilic substances, possesses an

orthorhombic packing at room temperature and the packing is transient at even slightly higher

temperatures. This lipid reorganization affects the transport properties of the skin for

hydrophilic substances. This fluidity in the lipid structure also forms the basis for the action

of penetration enhancers which help in transport of hydrophilic drug across the skin.

Topical delivery of drugs

Drugs incorporated in topical preparation may exert their effect in either due to the

pharmacological properties of the drug or due to the physicochemical characteristics of the

delivery system. The events occurring during the cutaneous absorption have been

schematically illustrated in figure 1.3.

Figure 1.3: Events of percutaneous absorption on drug.


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Gels have been extensively used as topical drug delivery systems for hydrophilic drugs.

Although gels possess certain advantages, such as greater dissolution of the drug, easy

migration of the drug through the matrix, faster onset of action than in the case of creams or

ointments, and better aesthetic appeal as compared oily formulations, they are not suitable

vehicles for hydrophobic molecules unless some solubility enhancer and/or an agent to modify

the intermolecular interactions is used.

Gel

Gels are defined as semi rigid systems in which the movement of the dispersing medium is

restricted by an interlacing three-dimensional network of particles or solvated macromolecules

of the dispersed phase. The initial idea of formulating gel was to set up a liquid to a solid- like

material that does not flow, but is elastic and retains some liquid characteristics. The rigidity

of a gel arises from the presence of a network formed by the interlinking of particles gelling

agent. The nature of the particles and the type of force that is responsible for the linkages,

which determines the structure of the network and the properties of the gel.

An ideal gel should be certain properties that might be related either to the gelling agent or

overall gel itself. The gelling agent must be inert and should be compatible to the other

formulation ingredients and it should possess solid structure until external force is applied. The

gel should be non sticky, sterile (if intended for ophthalmic use) and the components of the gel

must remain continuous throughout the system.

Formulation of gel

The formulation of pharmaceutical gel can be achieved by thermal changes, flocculation and

through chemical reaction. In thermal changes induced gelling, the solvated polymers

(lipophilic colloids) when subjected to thermal changes causes gelation. Many hydrogen

formers are more soluble in hot than cold water. If the temperature is reduced, the degree of

hydration is decreased and gelation takes place. (Cooling of a concentrated hot solution will

produce a gel).While using the flocculation method for preparing gel, gelation is produced by

adding just sufficient quantity of salt to precipitate to produce age state, but inadequate to

bring about complete precipitation. It is essential to ensure quick mixing to avoid local high

concentration of precipitant. In the chemical reaction induced gelation, the gelation of

materials is induced by the chemical interaction between the solute and the solvent.


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Evaluation of gels

The parameters that need to be characterized for any formulated gel include the measurement

of pH of the formulation, viscosity, drug content analysis, spreading ability, tube extrudation,

skin irritation test, in vitro diffusion, ex vivo diffusion, and in vivo study (if applicable). The

stability, grittiness and homogeneity of the formulation also need to be characterized.

The gel formulation may be launched in market for treatment or management of various

diseased states after the quality checks on the above characteristics as well as rigorous other

test conducted by the regulatory agencies. Some of the marketed formulations and a few

patented formulations are presented in table 1.1 and 1.2 respectively.

A few marketed gel formulations

S. no. Formulation

Name

API Gelling Agent Use

1 Voltaren

emulgel

Dicofenac

Sodium

Carbomer Muscle and back

pain

2 Metrogel Metronidazole Carbomer Antibacterial in

vaginal infections

3 Oxalgin nanogel Diclofenac

sodium, methyl

salicylate and

menthol

Carbomer Arthritis, low back

pain, muscular pain,

tennis elbow, sprains

and strains

4 Differin gel Adapalene Sodium CMC Acne treatment

5 Cleocin T Gel Clindamycin Carbomer Acne treatment

6 Aci-jel Acetic acid Tragacanth,

acacia

Restoration and

maintenance of

vaginal acidity

7 Ternovate Gel Clobetasol Carbomer 934 Antipruritic

8 Retin A Tretinion Hydroxypropyl

cellulose

Acne treatment

9 Desquam-X Gel Benzoly

peroxide

Carbomer 940 Acne treatment

Few of the patented gel formulation

S. no. Formulation intended for Patent No.

1 Topical gel delivery systems for treating skin disorders EP 1304992 B1

2 Hydrogel composition for transdermal drug delivery WO 0187276 A1

3 Topical antibiotic application EP 0183322 A2

4 Aqueous gel formulation for inducing topical anesthesia WO 2008014036A1

5 Stable gel formulation for topical treatment of skin

conditions

US 5914334 A


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Solid dispersion

The feasibility of administering a drug via a topical or transdermal route may incur several

difficulties that may result in unwanted side effects. Colloidal drug delivery systems have

arisen as popular approaches that can overcome these obstacles, thereby enhancing the drug

accumulation, absorption, and delivery to targeted sites. An effective colloidal formulation that

can be applied in skin delivery is a solid dispersion (SD), in which the drug is dispersed in inert

carriers. An SD has the ability to reduce the dispersed particle size, convert the drug from the

crystalline to the amorphous state, and augment its wetting capability, which greatly contribute

to the solubility improvement of poorly water-soluble drugs.

MATERIAL AND METHOD

Preformulation studies

Organoleptic evaluation: The color, odor and taste of the obtained drug sample were

observed with the help of the sensory organs.

Solubility (At room temperature, qualitative): Solubility was observed in different

solvents like water, HCl, ethanol and acetone.

Identification test: FT-IR spectrum of the sample of Griseofulvin was obtained and examined

for the presence of characteristic peaks and matched with that of the reference spectra in

databases for confirmation of the identity of the drug.

Melting point determination: Melting point was determined by open capillary method and is

uncorrected. A small quantity of powder was placed into fusion tube and placed in the melting

point apparatus. The temperature of the apparatus was gradually increased and the temperature

at which the powder started to melt and the temperature at which all the powder got melted

was recorded.

Compatibility analysis: The FTIR spectra of the pure drug and a physical mixture of the drug

and the polymers under study were obtained and observed for deletion of the characteristic

peaks of the drug.

Determination of λmax

Accurately weighed 5 mg of Griseofulvin was dissolved in 5 mL of methanol in a 10 mL

volumetric flask. 1 mL of this solution was taken in to a 10 mL volumetric flask and volume

made up to the mark with methanol.

400 nm using UV spectrophotometer. The λmax was found to be 295 nm. The solution was


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stored for 3 days at room temperature and rescanned to observe any changes in wavelength.

Preparation of calibration curve in methanol

Accurately weighed 10 mg of Griseofulvin was taken in 10 mL volumetric flask and dissolved

in methanol to the mark resulting in a stock solution of 1000 µg/mL. 1 mL of the above stock

solution was taken in another 10 mL volumetric and volume was made up with methanol to

mark resulting in a solution of 100 µg/mL. Aliquots of 1-6 mL of stock solution were taken

into a series of 10 mL volumetric flask and volume was made up to the mark using methanol

and were analyzed at 295 nm using UV spectrophotometer. A standard curve was constructed

against absorbance and concentration.

Formulation of solid dispersion of griseofulvin

The SD of griseofulvin was designed using I-optimal factorial approach, measuring the effect

of formulation variables on the measured responses. The independent variables for formulation

were the drug to polymer (D:P) ratio (X1) and the polymer type (X2). The chosen response for

measurement was the percentage dissolution efficiency at 15 min.

Design table for formulation of SD

Formulation SD1 SD2 SD3 SD4 SD5 SD6

X1 (D:P) 1:1 1:2 1:3 1:1 1:2 1:3

X2

(Polymer)

PVP

K30

PVP

K30

PVP

K30

Mannitol Mannitol Mannitol

The melting method was used for the preparation of solid dispersion. The drug and polymer

were mixed physically in a porcelain dish and heated on a paraffin bath till molten. The molten

mixture was poured on a clean tile and allowed to cool and solidify.[54]

The resulting

solidified mass was dried, finely ground in a mortal pestle and passed through sieve # 100.

Evaluation of griseofulvin SD

Drug content of solid dispersion

An accurately weighed 10 mg of the SD was taken in a 25mL volumetric flask and dissolved

in methanol by sonication for 15 min. The volume was made up to the mark with methanol. A

portion of the above solution was withdrawn and centrifuged for 10 min. 5 mL of the

supernatant was suitably diluted and analyzed spectrophotometrically at 295 nm.


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Solubility study

An excess amount of the SD was transferred to stoppered Erlenmeyer flask and 25 mL of

phosphate buffer pH 7.4 was added to it. The mixture was sonicated for 1 h and 2 mL of the

solution was withdrawn, filtered through Whatman filter paper no. 40 and analyzed

spectrophotometerically at 295 nm after appropriate dilution.

Dissolution study

Accurately weighed formulation from each batch, equivalent to 25 mg of griseofulvin was

added to 900 ml of dissolution media (phosphate buffer, pH 7.4) contained in USP

dissolution apparatus II (Paddle type) and stirred at a speed of 50 rpm at 37 ± 0.5°C. 5 mL of

sample were withdrawn at 5, 10, 15, 20 and 30 min and the medium was enriched with 5 ml of

fresh dissolution media (37°C). The collected samples were analyzed after suitable dilution at

295 nm using UV-visible spectrophotometer against the phosphate buffer, pH 7.4 as blank.

The dissolution of pure griseofulvin was studied similarly. The dissolution efficiency of SD

at 15 min was determined from the release data.

Formulation of SD loaded gel

Gel loaded with SD of griseofulvin were formulated using two gel forming polymers (Carbopol

934P and HPMC) using different concentration of the polymers and fixed amount of SD.

Gel formulation using carbopol

The accurately weighed quantity of the solid dispersion (table 2.4) was dispered in purified

water with constant stirring and the drug solution was heated to 50°C. The amount of carbopol

was added to the solution under continuous stirring while maintaining the temperature at 50°C

to ensure no air entrapment. The dispersion of the gelling agent was neutralized using

triethanolamine solution to neutral pH and the stirring was continued to obtain a clear gel.

Gel formulation using HPMC

The accurately weighed quantity of the solid dispersion (table 2.4) was dispered in purified

water with constant stirring and the drug solution was heated to 50°C. The amount of HPMC

was added to the solution under continuous stirring while maintaining the temperature at 50°C

to ensure no air entrapment. The dispersion of the gelling agent was neutralized using 10%

NaOH solution to neutral pH and the stirring was continued to obtain a gel.


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Evaluation of gel

Homogeneity

All the gel formulations were evaluated for homogeneity by visual inspection after the gels

were well set in the container. They were observed for their appearance and presence of any

aggregates.

Grittiness

All the formulations were evaluated under a light microscope for the presence of particlulate

matter. The absence of particles fulfills the criterion for a good gel formulation.

pH determination

1 gram of gel was dissolved in 100 ml of distilled water and allowed to stand for 2 h. The pH

of the resulting solution of each formulation was measured using digital pH meter in triplicate

and average values were calculated.

Viscosity

The measurement of viscosity of the prepared gel was done with a Brookfield Viscometer. The

gels were rotated at 20 rpm using spindle no. 64 and the corresponding dial reading was

recorded as the viscosity values. The viscosity was measured in centipoises (cp).

Rheological study

The gel formulations were subjected to shear stress (rpm) by rotating the spindle no. 64 at 10,

20, 40, 60, 80, and 100 rpm for 15 min and viscosity in centipoise was determined.

Spreadability

The spreadability of the gels was determined using Arvouet-Grand Method. Briefly, 1 g of

the gel was pressed between two 20 X 20 cm horizontal plates. A weight of 125 g is placed on

the upper plate for 1 min and diameter of spreading of gel was recorded. The spreadability of

formulations was measured in triplicate and the average value was determined.

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