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www.wjpps.com │ Vol 10, Issue 9, 2021. │ ISO 9001:2015 Certified Journal │
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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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