Formulation and Evaluation of Topical Acyclovir Gel Using Different Polymers
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Keywords

Acyclovir
carbopol-940
carboxymethylcellulose sodium
hydroxypropyl methylcellulose
in vitro drug release studies

Abstract

Background: Acyclovir is usually given as protracted therapy
and at greater dosing frequency for complete remittance of the
disease due to its low oral bioavailability, but this is associated
with side effects. Topical preparations of acyclovir are the
alternative route of administration to treat local dermatological
diseases caused by herpes simplex virus.
Objective: To prepare and evaluate the topical gel formulations
of acyclovir by using different polymers.
Materials and Methods: Acyclovir gels were formulated by
using three types of polymers, namely carboxymethylcellulose
sodium (CMC Na), hydroxypropyl methylcellulose (HPMC) and
carbopol-940 as gelling agents at different concentrations. They
were evaluated for several physicochemical characteristics
including physical appearance, grittiness, viscosity, spreadability,
pH, drug content uniformity and in vitro drug release studies. The
in vitro drug release of acyclovir from the selected gel
formulations was evaluated as per the procedure described in
United States Pharmacopoeia (USP), by using the standard 40mesh stainless steel dissolution basket (USP Apparatus 1)
containing cellulose acetate membrane with phosphate buffer pH
6.8 as the dissolution medium.
Results: Among all prepared gel formulations, formulation F8
containing 3% w/w of carboxymethylcellulose sodium was
selected as optimal gelling agent in acyclovir gel formulation due
to its desired physicochemical characteristics and it showed the
highest acyclovir in vitro release rate of 96.21 ± 0.92% over 5
hours.
Conclusion: The release of acyclovir from the gel formulations
was significantly affected by the type and concentration of
polymer (p-value < 0.05).

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References

James SH, Prichard MN. Current and Future Therapies for

Herpes Simplex Virus Infections: Mechanism of Action and

Drug Resistance. Current Opinion in Virology. 2014; 8: 54-

Cortesi R, Esposito E. Acyclovir Delivery Systems. Expert

Opinion on Drug Delivery. 2008; 5 (11): 1217-1230.

Patel S, Jain P, Parkhe G. Formulation and Evaluation of

Acyclovir Loaded Novel Nano-Emulsion Gel for Topical

Treatment of Herpes Simplex Viral Infections. Journal of

Drug Delivery and Therapeutics. 2018; 8 (5-s): 265–270.4. Satheesh Madhav NV, Ojha A. Labial Mucosa as a Novel

Transmucosal Drug Delivery Platform. International Journal

of Pharmacy and Pharmaceutical Sciences. 2012; 4 (3): 83-

Kikwai L, Babu RJ, Prado R, Kolot A, Armstrong CA, Ansel

JC, et al. In Vitro and In Vivo Evaluation of Topical

Formulations of Spantide II. AAPS PharmSciTech. 2005;

(4): E565-572.

Tanwar YS, Jain AK. Formulation and Evaluation of Topical

Diclofenac Sodium Gel Using Different Gelling Agent. Asian

Journal of Pharmaceutical Research and Health Care. 2012; 4

(1): 1-6.

Parchuri DB, Shantha Kumar GS, Goli D, Karki R.

Formulation and Evaluation of Nanoparticulate Drug

Delivery System of Acyclovir for Topical Drug Delivery.

World Journal of Pharmacy and Pharmaceutical Sciences.

; 2 (6): 5602-5617.

Helal DA, El-Rhman D, Abdel-Halim SA, El-Nabarawi MA.

Formulation and Evaluation of Fluconazole Topical Gel.

International Journal of Pharmacy and Pharmaceutical

Sciences. 2012; 4 (5): 176-183.

Garg A, Aggarwal D, Garg S, Singla AK. Spreading of

Semisolid Formulations: An Update. Pharmaceutical

Technology North America. 2002; 26 (9): 84-105.

United States Pharmacopoeia–National Formulary (USP37–

NF32). Vol. 1. Rockville (MD): United States Pharmacopeial

Convention; 2014. Physical Tests <711> Dissolution; p. 344.

Dongare US, Chemate SZ, Jadhav SA, Pawar VR.

Spectrophotometric Determination and Validation of

Acyclovir in Tablet Dosage Form. International Journal of

PharmTech Research. 2012; 4 (4): 1840-1845.

International Conference on Harmonisation (ICH) of

Technical Requirements for Registration of Pharmaceuticals

for Human Use. ICH, Q2 (R1) - Validation of Analytical

Procedures: Text and Methodology. Geneva, Switzerland:

ICH Harmonised Tripartite Guideline; 2005.13. Kumar BK, Thiruvengada Rajan VS, Begum NT. Analytical

Method Development and Validation of Lidocaine in

Ointment Formulation by UV Spectrophotometric Method.

International Journal of Pharmacy and Pharmaceutical

Sciences. 2012; 4 (2): 610-614.

Macedo T, Block LH, Shukla AJ. Release of Tolmetin from

Carbomer Gel Systems. Drug Development and Industrial

Pharmacy. 2008; 19 (8): 887-902.

Kaur LP, Garg R, Gupta GD. Development and Evaluation of

Topical Gel of Minoxidil from Different Polymer Bases in

Application of Alopecia. International Journal of Pharmacy

and Pharmaceutical Sciences. 2010; 2 (3): 43-47.

Farage MA, Hood W, Berardesca E, Maibach H. Intrinsic and

Extrinsic Factors Affecting Skin Surface pH. Current

Problems in Dermatology. 2018; 54: 33-47.

United States Pharmacopoeia–National Formulary (USP37–

NF32). Vol. 2. Rockville (MD): United States Pharmacopeial

Convention; 2014. Official Monographs: Acyclovir; p. 1616.

Kaur D, Raina A, Singh N. Formulation and Evaluation of

Carbopol 940 Based Glibenclamide Transdermal Gel.

International Journal of Pharmacy and Pharmaceutical

Sciences. 2014; 6 (8): 434-440.

Taş C, Ozkan Y, Savaşer A, Baykara T. In Vitro and Ex Vivo

Permeation Studies of Chlorpheniramine Maleate Gels

Prepared by Carbomer Derivatives. Drug Development and

Industrial Pharmacy. 2004; 30 (6): 637-647.

United States Pharmacopoeia–National Formulary (USP37–

NF32). Vol. 1. Rockville (MD): United States Pharmacopeial

Convention; 2014. General Information <1092> The

Dissolution Procedure: Development and Validation; p. 8

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