Formulation, Development and Evaluation of Nasal In situ Gel of Pregabalin

DOI:

https://doi.org/10.37285/ijpsn.2021.14.5.5

Authors

  • Anuradha P Prajapati epartment of Pharmaceutics, Smt. B.N.B Swaminarayan Pharmacy College, Salvav-Vapi. 396191, Gujarat, India.
  • Jalpa H Kanzaria Department of Pharmaceutics, Smt. B.N.B Swaminarayan Pharmacy College, Salvav-Vapi. 396191, Gujarat, India.
  • Shailesh V Luhar Department of Pharmaceutics, Smt. B.N.B Swaminarayan Pharmacy College, Salvav-Vapi. 396191, Gujarat, India.
  • Sachin B Narkhede Department of Pharmaceutics, Smt. B.N.B Swaminarayan Pharmacy College, Salvav-Vapi. 396191, Gujarat, India.

Abstract



The objective of the present work is to formulate, develop and evaluate nasal in situ gel of Pregabalin to provide better therapy for Epilepsy. Pregabalin is BCS class I drug. It is 3rd generation anticonvulsant used in epilepsy in which faster action is required. Nasal route has faster action than oral route, also convenient to unconscious patient. Pregabalin loaded in situ gel, for the treatment of epilepsy to avoid side effects and first pass metabolism associated with conventional treatment and increase bioavailability. Pregabalin was loaded into different polymeric solutions of Polycarbophil and HPMC K4M. The drug was characterized for various parameters like UV-Spectroscopy, FTIR Spectroscopy and DSC study. Excipients were screened for selection of mucoadhesive and gelling polymer. Then the drug was formulated as in situ gel. The experiment was subjected to 32 full factorial design, the concentration of Polycarbophil (X1) and HPMC K4M (X2) were selected as independent variables with % drug release and muco-adhesive strength as dependent variables. The kinetic study was carried out for 30 days. Polycarbophil was selected as mucoadhesive and gelling polymer. The values for X1 and X2 were 0.3922% and 0.5263% relating the % drug release and mucoadhesive strength values were 78.20% CDR at 240 min. and 960 dynes/cm2 respectively for checkpoint batch following zero order and Higuchi kinetic. The formulation was found to be stable for 30 days. The present research will be helpful in order to improve the efficacy and tolerability of the antiepileptic drug therapy. So alternative administration strategy has been investigated which deliver nasally administered medication directly to brain effectively. The intranasal in situ gelling system is a promising novel drug delivery system for an antiepileptic drug Pregabalin which could enhance nasal residence time with increased viscosity and mucoadhesive character and provided better release profile of drug for treating epileptic conditions.  

Downloads

Download data is not yet available.

Metrics

Metrics Loading ...

Keywords:

Epilepsy, Intranasal Route, Pregabalin, Nasal In Situ Gel

Downloads

Published

2021-09-01

How to Cite

1.
Prajapati AP, Kanzaria JH, Luhar SV, Narkhede SB. Formulation, Development and Evaluation of Nasal In situ Gel of Pregabalin . Scopus Indexed [Internet]. 2021 Sep. 1 [cited 2024 Dec. 22];14(5):5612-24. Available from: https://ijpsnonline.com/index.php/ijpsn/article/view/2212

Issue

Section

Research Articles

References

K.D. Tripathi (2013). Essentials of Medical Pharmacology. 7th Edn; Jaypee Brothers, India, 411-424.

R. S. Satoskar, S. D. Bhandarkar and Nirmala N (2009). Pharmacology and Pharmacotherapeutics 20th Edn, 135.

Marvin M. Goldenberg (2010). Overview of Drugs Used For Epilepsy and Seizures Etiology, Diagnosis, and Treatment. July 35(7): 392–415.

Anthony J. Trevor and Bertram G. Katzung (2015). Marieke Kruidering-Hall. Katzung And Trevor’s Pharmacology Examination And Board Review; 11th Edn : 201-207.

Barbara R. Conway and Muhammad U. Ghori (2015). Nasal Drug Delivery Systems: An Overview. Amer J Pharm Sci 3(5): 110-119.

M.Alagusundara (2010). Nasal drug delivery system - an overview. Int J Res Pharm Sci 1(4): 454-465.

S. Upadhyay (2011). Intranasal drug delivery system- A glimpse to become maestro. J App Pharm Sci 01(03): 34-44.

Chand (2016). In situ gel: A Review. Ind J Pharm and Bio Res 4(2): 11-19.

Bajpai Vibha (2014). In-Situ Gel Nasal Drug Delivery System-A Review. Int J Pharm Sci 4(3): 577-580.

Mayuri M. Ban (2018). In-situ gel for nasal drug delivery. Int J Dev Res 8(02):18763-18769.

Gupta K (2015). Drug excipient compatibility study using thermal and non-thermal methods of analysis. Int J Chem App 2(2): 23- 49.

International Conferences on Harmonization (ICH) (2005). Validation of analytical procedure, Text and Methodology, Harmonized tripartile guideline. Q2 (R1), Geneva.

Boltan S and Bon C (2005). Pharmaceutical Statistics Practical and Clinical Applications,4th Ed. Marcel Dekker, New York.

Lewis G.A. and Mathieu D (1999). The scope of Experimental Design, Pharmaceutical Experimental Designs, Marcel Dekker, New York.

Banker G.S. and Rhodes C. T (1988). Modern Pharmaceutics, 4th Ed. Marcel Dekker, New York: 607-625.

P R Patil (2015). Formulation and Evaluation of Ion-Sensitive In-Situ Nasal Gel of Zolmitriptan. Int J Pharm Sci 7(1): 478-486.

V.S. Belgamwar (2009). Formulation and evaluation of in situ gelling system of dimenhydrinate for nasal administration. Pharm Dev Tech 14(3): 240-248.

Suvakanta Dash (2010). Kinetic Modeling On Drug Release From Controlled Drug Delivery Systems. Acta Poloniae Pharm 67(3): 217-223.

International Conferences on Harmonization (ICH) Topic Q1A (R2) stability testing guideline: Stability testing of new drug substances and products.

Raghavendra Kumar Gunda and J. N. Suresh Kumar (2015). Formulation development and evaluation of Zidovudine sustained release tablets using 32 factorial design. Der Pharm Sinica 6(6): 59-67.

J. Hao (2016). Fabrication of an ionic-sensitive in situ gel loaded with resveratrol nanosuspensions intended for direct nose-to-brain delivery. Elsevier- Coll Sur B: Biointer 147: 376-386.

Patil Sonali (2015). Formulation and evaluation of nasal in situ gel for Alzheimer disease. Int Res J Pharm and Biosci 2(2): 41- 58.

Blessing A and tim Aderibigbe (2018). In Situ-Based Gels for Nose to Brain Delivery for the Treatment of Neurological Diseases. MDPI-Pharm 10(40): 1-17.

A.R. Khan (2017). Progress in brain targeting drug delivery system by nasal route. Elsevier-J Cont Rel 2(68): 364–389.

Walter H. Hsu (2017). Mechanism of intranasal drug delivery directly to the brain. Life Sciences. 1-28.

M Marjani (2015). Comparison of intranasal and intramuscular ketamine midazolam combination in cats. Vet Anaes Ana 42: 178–181.

Charles P. Taylora, Timothy Angelotti and Eric Fauman (2007). Pharmacology and mechanism of action of pregabalin: The calcium channel α2-δ (alpha2—delta) subunit as a target for antiepileptic drug discovery. Elsevier - Epilepsy Research 73: 137-150.

Heidrun Potschka (2013). Pharmacological treatment strategies: Mechanisms of antiepileptic drugs. Elsevier –Epileptology 1(1): 31-37.

Christina Karavasili and Dimitrios G. Fatouros (2015). Smart materials: in situ gel-forming systems for nasal delivery. Elsevier- Drug Dis Today. 1-10.

Wallace H, Shorvon S. and Tallis R (1998). Age-specific incidence and prevalence rates of treated epilepsy in an unselected population of 2,052,922 and age-specific fertility rates of women with epilepsy. Lancet. 352(9145):1970–1973.