Chapter II Literature Review
2. LITERATURE SURVEY
2.1 Review of literature:
Rachit khullar et al., 2021 was formulated and evaluated mefenamic acid emulgel
for topical delivery using carbapol 940 as a gelling agent. Mefenamic acid emulsion
was prepared and it was incorporated in gel base. The formulations were evaluated for
rheological studies, spreading coefficient studies, skin irritation studies, in vitro
release, ex vivo release studies, anti inflammatory and analgesic activity. And
concluded that topical emulgel of mefenamic acid posses an effective anti
inflammatory and analgesic activity32.
El Laithy HM et al., 2021 was studied the influence of the vehicle on the release and
permeation of fluconazole, a topical antifungal drug dissolved in Jojoba oil was
evaluated. Series of Cutina lipogels (Cutina CPA [cetyl palmitate], CBS [mixture of
glyceryl stearate, cetearyl alcohol, cetyl palmitate, and cocoglycerides], MD [glyceryl
stearate], and GMS [glyceryl monostearate]) in different concentrations as well as gel
microemulsion were prepared. In-vitro drug release in Sorensen's citrate buffer (pH
5.5) and permeation through the excised skin of hairless mice, using a modified Franz
diffusion cell were performed. The results of in vitro drug release and its percutaneous
absorption showed that the highest values from gel micro emulsion were assured33.
Gupta M et al., 2021 prepared a meloxicam gel using different polymers as gelling
agent in varied concentrations. Polymers such as carbopol 940NF (0.2-1.0% w/v),
carbopol 941 (0.2-1.0% w/v), carboxymethylcellulose sodium (3-5% w/v) and
methylcellulose (6-8% w/v) were selected for preparation of gel. The prepared gels
were evaluated for in-vitro release of drug and anti-inflammatory activity.
Formulation A (carbopol 940; 0.2% w/v), B (carbopol; 0.4%w/v), F (carbopol 940;
02%w/v) and K (carboxymethylcellulose sodium; 3% w/v) were found to be the best
formulation34.
Yesim karasulu et al., 2021 was formulated and evaluated the skin permeation and
anti-inflammatory and analgesic effects of new naproxen microemulsion
formulations. The microemulsions were characterized by conductivity, droplet size,
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Chapter II Literature Review
viscosity and pH and concluded that microemulsion formulations may be used as an
effective alternative for the transdermal delivery of naproxen35.
Praveen Khandre et al., 2020 carried out formulation and evaluation studies on
nimesulide topical gel using carbopol and HPMC polymers. And concluded that
nimesulide topical gels of carbopol polymers showed better spreadability, rheological
behaviour and good anti-inflammatory activity when compared to marketed
formulation of nimesulide topical gel36.
Doaa Ahmed et al., 2010 was prepared ketorolac trometamol emulgel using
isopropyl myristate, isopropyl palmitate, Tween 80, oleic acid, transcutol, propyl
glycol, glycerin, water. In-vitro release behaviour of the drug from different
microemulsion and emulgel formulations was evaluated. The developed emulgel
appeared promising for dermal and transdermal delivery of ketorolac trometamol,
which would circumvent most of the problems associated with drug therapy37.
Piyusha Deveda et al., 2020 was formulated gellified emulsion for sustained delivery
of itraconazole. The prepared formulations were evaluated on the basis of pH,
spreadability, viscosity, drug content, in vitro drug release and stability studies. The
microbial assay and skin irritation studies on rabbit was also performed. It was
concluded that emulsion based system was more effective and safe system for
sustained delivery of itraconazole38.
Madhu Madan et al., 2019 was developed an emulgel formulation for a local
anesthetic agent and a topical steroidal anti-inflammatory agent in combination using
sepigel as the gelling agent. The effect of concentrations of oil, surfactant and gelling
agent on the in vitro drug release pattern was investigated using 23 factorial design.
The optimized emulgel formulations were characterized for appearance, color, pH,
homogenecity, viscosity and spreadability. The rheological property of emulgels
showed shear thinning behaviour with thixotropy. The drug release from the
optimized emulgel formulation was found to follow the diffusion controlled Higuchi
model. Stability studies were conducted at different temperatures and humidity
conditions that indicated the formulations to be stable under accelerated conditions.
No erythema or irritation was observed during the skin irritation studies on rabbits.
The result obtained was considered as a step forward for the prolonged topical
delivery of drugs in combination for the treatment of various skin disorders39.
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Chapter II Literature Review
Manli Wang et al., 2018 the study was conducted to evaluate the permeation of
diclofenac acid and its salts from emulgel. Emulgel was prepared by dispersing
carbomer 974 in purified water and adding triethanolamine to adjust the viscosity.
Their penetration performances were evaluated using two-chamber side-by-side
diffusion cells containing excised rat skin and the drug concentration in the receptor
compartment was determined by HPLC. The partition coefficient of the drugs
between stripped skin and emulgel (Ks) was also determined and a positive
relationship was found between Ks and the cumulative amount of drug permeated
over a period of 8 h with a correlation coefficient (r) of 0.974. So it was concluded
that Diclofenac salts were more suitable for emulgel preparation than diclofenac free
acid40.
Ana Amelia M. et al., 2018 was developed a topical formulation of lapachol, a
compound isolated from various Bignoniaceae species and evaluating its topical anti-
inflammatory activity. The influence of the pharmaceutical form and different types
of emulsifiers was evaluated by in-vitro release studies. The formulations showing the
highest release rate were selected and assessed through skin permeation and retention
experiments. It was observed that the gel formulation provided significantly higher
permeation and retained (3.9-fold) of lapachol as compared to the cream formulation.
Moreover, lapachol gel presented significant antiedematogenic and antinociceptive
activities when used topically. Hence, these results suggest that the topical delivery of
lapachol from gel formulations can be an effective medication for topical injuries41.
Rhee. Y. S et al., 2018 developed a transdermal gel formulation for ibuprofen using
experimental design techniques to evaluate its pharmacokinetic properties. The three
factors chosen for factorial design were the concentration of drug wherein the levels
of each factor were low, medium and high. Skin permeation rates and lag times of
ibuprofen were evaluated using the Franz-type diffusion cell in order to optimize the
gel formulation. The pharmacokinetic properties of the optimized formulation were
compared with those of two marketed products in rats. It was concluded that a
transdermal ibuprofen gel could be formulated using the technique of experimental
design42.
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Chapter II Literature Review
Dongsheng Mou et al., 2018 Hydrogel-thickened nano-emulsion systems (HTN)
with powerful permeation ability, good stability and suitable viscosity was
investigated for topical delivery of active molecules. HTN was prepared to deliver an
oily mixture of 5% camphor, 5% menthol and 5% methyl salicylate for topical
therapy of arthritis, minor joint and muscle pain using soybean oil as the oil phase,
soybean lecithin, Tween 80 and poloxamer 407 as the surfactants, propylene glycol as
the cosurfactant, carbomer 940 as a thickening agent43.
Moti L Tiku et al., 2017 Glucosamine sulphate as a putative agent that may retard
cartilage degradation in osteoarthritis was investigated. The effect of glucosamine in
an in vitro model of cartilage collagen degradation in which collagen degradation
induced by activated chondrocytes is mediated by lipid peroxidation reaction. Lipid
peroxidation in chondrocytes was measured by conjugated diene formation. Protein
oxidation and aldehydic adduct formation were studied by immunoblot assay.
Antioxidant effect of glucosamine was also tested on malondialdehyde formation on
purified lipoprotein oxidation for comparision. Finally it was concluded that in an in
vitro cartilage collagen degradation in which collagen degradation induced by
activated chondrocytes is mediated by lipid peroxidation reaction, glucosamine
decreased collagen degradation by inhibiting advanced lipoxidation reaction and thus
prevents the oxidation and loss of collagen matrix from Labeled chondrocyte matrix44.
Isik Sarigullu Ozguney et al., 2016 the study was conducted to evaluate and
compare the in vitro and in vivo transdermal potential of w/o microemulsion and gel
bases for diclofenac sodium. The effect of dimethyl sulfoxide (DMSO) as a
penetration enhancer was also examined. To study the in vitro potential of these
formulations, permeation studies were performed with Franz diffusion cells using
excised dorsal rat skin. To investigate their in vivo performance, a carrageenan-
induced rat paw edema model was used. This study demonstrated that incorporating
drug into microemulsion enhanced drug penetration through rat skin in vitro and in
vivo45.
Department of Pharmaceutics, SKIPSc 18
