Introduction
• Inflammation: Immune response to tissue injury or infection, driven by
mediators .
• Global Impact: Inflammation and pain affect millions globally,
contributing to disability, decreased productivity, and rising healthcare
costs.
• Prevalent Conditions: Major conditions like rheumatoid arthritis,
inflammatory bowel disease, and COPD affect over 1.7 billion people
globally, especially in low- and middle-income countries.
• Opioid Crisis: Increased opioid-related deaths highlight the need for better
pain management strategies, especially in countries with liberal prescribing
practices.
• NSAIDs: Inhibit COX enzymes, reducing prostaglandin synthesis and
alleviating pain/inflammation.
• Traditional NSAIDs: Effective but associated with gastrointestinal and
cardiovascular risks
• Most traditional NSAIDs are poorly water-soluble and good permeability
across biological membranes, allowing for effective absorption, but their
low solubility can limit bioavailability.
• Solid dispersion represents a promising strategy in pharmaceutical science
for enhancing the solubility, bioavailability, and therapeutic efficacy of
poorly water- soluble drugs.
Rationlae of the study
• Aceclofenac, classified as a BCS class II drug with 3.5µg/ml solubilty and
log p 2.1 resulting in low oral bioviavailbilty.
• Its its topical absorption is hindered by limited dissolution in aqueous
environments.
• Overcoming these challenges requires innovative formulation strategies
tailored to enhance solubility, permeability, and localized efficacy, while
minimizing systemic exposure and variability in drug response.
• The study aims to develop and evaluate a gel formulation of aceclofenac
using solid dispersion with biocompatible polymers for enhanced topical
delivery, focusing on its biopharmaceutical performance compared to
commercially available formulations
Drug characterstics
Class Pharmacokinitc Dosage Mechanisim of
action
Aceclofenac is a It is rapidly
non-steroidal absorbed after oral The recommended Mechanism of
anti-inflammatory administration, dosage of aceclofenac Action: Aceclofenac
drug (NSAID) achieving peak for adults is typically inhibits
belonging to the plasma 100 mg administered cyclooxygenase
phenylacetic acid concentrations twice daily, depending (COX) enzymes,
derivative class. within 1.25 to 3 on the severity of the reducing
hours, with a half- condition and patient prostaglandin
life of 4-4.3 hours, response synthesis, which
and is primarily leads to decreased
metabolized in the inflammation, pain,
liver to its active and swelling in
metabolite, with inflammatory
excretion mainly conditions.
via urine.
AIM:
• To formulate the solid dispersion based
Aceclofenac Loaded Gel For The Management
Of inflammation and pain.
• To evaluate the successful batches of
Aceclofenac gel against candida albicans
based Onychomycosis
Plan of work
• Conducted pre-formulation studies using FTIR and DSC to assess the
morphology, physicochemical properties, and drug-excipient compatibility
of aceclofenac.
• Fabricated solid dispersions of aceclofenac to enhance solubility and
bioavailability, characterized through advanced techniques.
• Incorporated solid dispersions into a gel matrix, evaluating drug release,
stability, and viscosity to improve therapeutic efficacy in inflammation and
pain management.
• In vitro assays demonstrated significant drug release of the aceclofenac gel
formulation, highlighting the benefits of solid dispersion technology.
API Lipids Excipients Aceclofenac and biocompatible
polymers (e.g., PVP K30, PEG
4000, Urea) were chosen for solid
dispersion formulation.
Aceclofenac Poly vinyl Methanol
pyrollidone Aceclofenac-loaded solid
dispersions were prepared via
Polyethylene Triethanolami solvent evaporation, incorporating
glycol ne the drug into polymers melted at
45-160°C.
Urea Distilled
Water
Carbopol was dispersed in water
under continuous stirring until
fully hydrated, followed by
Potassium neutralization to the desired pH,
Carbopol 934 di hydrogen resulting in a smooth, homogenous
phosphate gel base.
Di-sodium Solid dispersions were integrated
into a gel base. carbopol 934 and
hydrogen mixed thoroughly to achieve the
phosphate desired pH, consistency, and
spreadability for topical
application.
• Standardization of ACK by UV
• UV Spectrum of ACK sample showed maximum absorption at 274nm
which was consistent with reference value.
• FTIR spectrum of Aceclofenac
• The structure of Aceclofenac was identified from functional group thus
sample was pure.
• DSC thermogram showed a sharp endotherm(indicating Amorphous
state) at 160.11°C.
• Consistent with the standard melting temperature, indicating sample purity.
1.0 1.0
f(x) = 0.0373096774193549 x − 0.0319225806451615 f(x) = 0.0348650537634409 x − 0.0180129032258065
Absorbance (nm)
R² = 0.998183157575712 0.8 R² = 0.999803863223397
0.8
Absorbance (nm)
0.5
0.5
0.3
0.3
0.0
0.0 0 5 10 15 20 25
0 5 Concentration
10 (µg/ml)
15 20 25 Concentration (µg/ml)
100.000
75.000
50.000
25.000
ACKSD11 ACKSD12 ACKSD13 ACPSD11 ACPSD12 ACPSD13 ACUSD11 ACUSD12 ACUSD13
% Drug Content % Yield
100
% Cumulative Drug Release
75
50
25
0
0 2.5 5 7.5 10
Time (h)
ACF ACKPM11 ACKSD11G ACKSD12G AMF
summary
• Preformulartion studies on ACK showed melting point 160.11˚C,
exothermic sharp peak at --- in DSC studies and characterstic absorption
peaks at--------------and----------- for the presence of groups such
as------------- in FTIR spectral studies respectivily . Further X-Ray
diffraction data also recived for purity of drug similar to DSC and FTIR
studies.
• For the quantative analysis of PCZ as an analytical method based on UV
spectroscopy in methanol and phosphate buffer 5.5 respectively established
linearly with r value of 0.9982 and 0.9998 and obeyed Beer lambert law.
• Drug exciepient compatibilty was checked by using FTIR of ACK with
various formulations exciepients confirmed that the ACK maintained its
chemical integirity in presence of chosen polymers and exciepients.
