PREFORMULATION STUDIES OF PILOCARPINE HYDROCHLORIDE AS NIOSOMAL GELS FOR OCULAR DRUG DELIVERY

NEELAM JAIN; ANURAG VERMA

doi:10.22159/ajpcr.2020.v13i6.37523

Authors

NEELAM JAIN Department of Pharmacy, Oriental College of Pharmacy and Research, Oriental University, Indore, Madhya Pradesh, India.
ANURAG VERMA Department of Pharmacy, School of Pharmaceutical Sciences, IFTM University, Moradabad, Uttar Pradesh, India.

DOI:

https://doi.org/10.22159/ajpcr.2020.v13i6.37523

Keywords:

Pilocarpine hydrochloride, Preformulation, Ocular delivery, Spectrometric analysis, Compatibility

Abstract

Objective: Pilocarpine hydrochloride is a direct acting cholinergic parasympathomimetic agent which directly stimulates cholinergic receptor (M3). It is a drug used in the treatment of chronic open-angle glaucoma for over 100 years. Designing a new ophthalmic dosage form for pilocarpine hydrochloride compels performing preformulation studies for drug. Therefore, the current aim of the study was to investigate some of the important physicochemical properties of pilocarpine hydrochloride which can help to select subsequent approaches during the development of niosomal gel for ocular use.

Methods: Preformulation studies of drug were carried out for identification (physical appearance, melting point, and UV spectrophotometric analysis), solubility profile, lipophilicity (partition coefficient), compatibility studies by Fourier-transform infrared (FTIR) spectroscopy, and thermal behavior by differential scanning calorimetry (DSC).

Results: The melting point of pilocarpine hydrochloride was found to be 204 ± 3○C. The log P value was found to be 1.12 ± 0.02, from which it can be interpreted that drug is highly hydrophilic in nature. The scanned λmax was found to be 215 nm. No significant changes were found when FTIR spectra of physical mixture compared with FTIR spectra of pure drug and excipients. This indicates absence of any possible interaction between the drug and excipients which confirms the identity and purity of drug. DSC thermogram of pure drug showed a sharp exothermic peak at 191.923○C (area=68.890 mJ, delta H = 22.963 J/g), indicating the crystal melting point of the drug.

Conclusion: These results suggest that the pilocarpine hydrochloride serves as suitable candidate for ocular drug delivery system.

Downloads

Download data is not yet available.

References

Aulton ME. Aulton’s Pharmaceutics: The Design and Manufacture of Medicines. 3rd ed. London, United Kingdom: Churchill livingstone; 2007.

Rosin A. Pilocarpine: A miotic of choice in the treatment of glaucoma has passed 110 years of use. Oftalmologia 1991;35:53-5.

Khaw PT, Shah P, Elkington AR. Glaucoma-2: Treatment. BMJ 2004;328:156-8.

Jain N, Verma A, Jain N. Niosomes encapsulated pilocarpine hydrochloride for ocular controlled delivery. Int J Pharm Bio Sci 2019;9:813-23.

Available from: https://www.drugbank.ca/drugs/DB01085.

Jain N, Verma A, Jain N. Anti-glaucomatic niosomal gel: A brief review. World J Pharm Pharm Sci 2020;9:529-48.

Tomar S, Singhal T. Preformulation studies of niosomal gel of prednisolone and azithromycin for topical drug delivery system. J Innov Pharm Biol Sci 2015;2:312-21.

United States Pharmacopeia-National Formulary. The Official Compendia of Standards. United States: United States Pharmacopeial Commission; 2007.

Jayanthi B, Madhusudhan S. Preformulation characterisation, designing and formulation of aceclofenac loaded microparticles. Int J Drug Dev Res 2012;4:186-96.

Lachman L, Lieberman HA, Kanig JL. The theory and practice of industrial pharmacy. 3rd ed. Ernakulam: Varghese Publishing House; 1986.

Berthod A, Broch SC. Determination of liquid-liquid partition coefficients by separation methods. J Chromatogr A 2004;1037:3-14.

Meylan WM, Howard PH. Atom/fragment contribution method for estimating octanol-water partition coefficients. J Pharm Sci 1995;84:83-92.

Jain N, Banik A, Gupta A. Novel interpenetrating polymer network microspheres of lepidium sativum and poly(vinyl alcohol) for the controlled release of simvastatin. Int J Pharm Pharm Sci 2013;5:125-30.

Jain N, Kumar H, Rajpoot AK, Verma HC. Novel interpenetrating polymer network mucoadhesive microspheres of locust bean gum and poly(vinyl alcohol) for the delivery of famotidine. MIT Int J Pharm Sci 2015;1:27-36.

Jain N, Verma A, Jain N. In vitro evaluation of niosomal gel containing pilocarpine hydrochloride for ocular delivery. Lat Am J Pharm 2020;39:431-8.

Schoenwald RD, Huang HS. Corneal penetration behavior of beta blocking agents I: Physichochemical factors. J Pharm Sci 1983;72:1266-72.