Author(s): Reema B. Gotmare, R. S. Kushwaha, Neeraj K. Sharma

Email(s): Email ID Not Available

DOI: 10.52711/0975-4377.2021.00047   

Address: Reema B. Gotmare, R. S. Kushwaha, Neeraj K. Sharma
Department of Phramaceutics, Patel College of Pharmacy, Ratibad, Bhopal-462044.
*Corresponding Author

Published In:   Volume - 13,      Issue - 4,     Year - 2021


ABSTRACT:
Tapentadol Hydrochloride is a Tapentadol is a centrally acting analgesic. It has 33% bioavailability due to its first pass effect and hence possesses problems in the development of oral sustained release formulations. Mucoadhesive thermo reversible in-situ nasal gel of Tapentadol HCl was designed and developed to sustain its release due to the increased nasal residence time of the formulation. Poloxamer 407 (PF 127) was selected as it has excellent thermo sensitive gelling properties. HPMCK4M was added to impart mucoadhesive to the formulation, and PEG 400 was used to enhance the drug release. 32 Factorial designs were employed to assess the effect of concentration of HPMCK4M and PEG 400 on the performance of in-situ nasal gel systematically and to optimize the formulation. An optimized in-situ nasal gel was evaluated for appearance, pH, drug content, gelation temperature, mucoadhesive force, viscosity and ex-vivo permeability of drug through nasal mucosa of a goat. Additionally, this formulation was proved to be safe as histopathological studies revealed no deleterious effect on nasal mucosa of a goat after prolonged exposure of 21 days to the optimized formulation. Thus the release of Tapentadol Hydrochloride can be sustained if formulated in an in-situ nasal gel containing poloxamer 407 to achieve its prolonged action.


Cite this article:
Reema B. Gotmare, R. S. Kushwaha, Neeraj K. Sharma. Formulation and Evaluation of Mucoadhesive in-Situ Nasal Gel of Tapentadol Hydrochloride. Research Journal of Pharmaceutical Dosage Forms and Technology. 2021; 13(4):285-1. doi: 10.52711/0975-4377.2021.00047

Cite(Electronic):
Reema B. Gotmare, R. S. Kushwaha, Neeraj K. Sharma. Formulation and Evaluation of Mucoadhesive in-Situ Nasal Gel of Tapentadol Hydrochloride. Research Journal of Pharmaceutical Dosage Forms and Technology. 2021; 13(4):285-1. doi: 10.52711/0975-4377.2021.00047   Available on: https://rjpdft.com/AbstractView.aspx?PID=2021-13-4-4


REFERENCES:
1.    Yasir M and Sara UVS: Nose to brain drug delivery: A novel approach through solid lipid nanoparticles. Current Nanomedicine 2016; 6(2): 105-132.
2.    Lochhead JJ: Hypoxic stress and inflammatory pain disrupt blood-brain barrier tight junctions: implications for drug delivery to the central nervous system. The AAPS Journal 2017; 19(4): .910-920.
3.    Lim ST, Martin GP, Berry DJ and Brown MB: Preparation and evaluation of the in-vitro drug release properties and mucoadhesion of novel microspheres of hyaluronic acid and chitosan. Journal of Controlled Release 2000; 16(2-3): 281-92.
4.    Altunas E and Yener G: Formulation and evaluation of thermoreversible in situ nasal gels containing mometasone furoate for allergic rhinitis. AAPS Pharma Sci-Tech 2017; 18(7): 2673-2682.
5.    Shelke S, Shahi S, Jadhav K, Dhamecha D, Tiwari R and Patil H: Thermoreversible nanoethosomal gel for the intranasal delivery of Eletriptan hydrobromide. Journal of Materials Science: Materials in Medicine 2016; 27(6):103.
6.    Mali KK: Nasal Mucoadhesive in-situ gel of granisetron hydrochloride using natural polymers. Journal of Applied Pharmaceutical Science 2015; 5: 084-093.
7.    Kaur P, Garg T, Rath G and Goyal A: In-situ nasal gel drug delivery: A novel approach for brain targeting through the mucosal membrane. Artificial cells, Nanomedicine, and Biotechnology 2016; 44(4): 1167-76.
8.    Pardeshi CV and Belgamwar VS: Direct nose to brain drug delivery via integrated nerve pathways bypassing the blood–brain barrier: an excellent platform for brain targeting. Expert Opinion on Drug Delivery 2013; 10(7): 957-72.
9.    Kanazawa T, Kaneko M, Niide T, Akiyama F, Kakizaki S, Ibaraki H, Shiraishi S, Takashima Y, Suzuki T and Seta Y: Enhancement of nose-to-brain delivery of hydrophilic macromolecules with stearate-or polyethylene glycol-modified arginine-rich peptide. International Journal of Pharmaceutics 2017; 530(1-2): 195-200.
10.    Gizurarson S: The effect of cilia and the mucociliary clearance on successful drug delivery. Biological and Pharmaceutical Bulletin 2015; 38(04): 497-506.
11.    Sallam MA, Helal HM and Mortada SM: Rationally designed nanocarriers for intranasaltherapy of allergic rhinitis: influence of carrier type on in-vivo nasal deposition. International Journal of Nanomedicine 2016; 11: 2345.
12.    Farooqui S, Zahid M, Parveen S, Ahmad Z, Singh P and Parveen Z: Alzheimer's disease: delivery of the drug through intranasal route. Journal of Drug Delivery and Therapeutics 2016; 6(6): 60-69.
13.    Jaiswal N: Scope of Nasal Drug Delivery: Current Challenges. World Journal of Medical Sciences 2017; 14(4): 97-112.
14.    Menzel C and Jelkmann M. Nasal drug delivery: design of a novel mucoadhesive and in-situ gelling polymer. International Journal of Pharmaceutics 2017; 517(1-2): 196-202.
15.    Kumar H: Intranasal drug delivery: a non-invasive approach for the better delivery of neurotherapeutics. Pharmaceutical Nanoparticle 2017; 5(3): 203-214.
16.    Vibha B: In-situ gel nasal drug delivery system-a review. International Journal of Pharma Sciences 2014; 4(3): 577-80.
17.    Paul A, Fathima KM and Nair SC: Intra nasal in-situ gelling system of lamotrigine using ion activated mucoadhesive polymer. The Open Medicinal Chemistry Journal 2017; 11: 222.
18.    Khairnar S, Singh AK, Darekar A and Saudagar R: An innovative approach for in-situ gelling system for Nasal drug delivery: an overview. World Journal of Pharmaceutical Sciences 2015; 4(1): 334-56.
19.    Waldman HJ: Centrally acting skeletal muscle relaxants and associated drugs. Journal of pain and symptom management 1994; 9(7): 434-41.
20.    Brioschi TM, Schramm SG, Kano EK, Koono EE, Ching TH, Serra CH and Porta V: Pharmacokinetics and bioequivalence evaluation of cyclobenzaprine tablets. BioMed research international 2013; 5(4): 78-89.
21.    Patel D, Naik S, Chuttani K, Mathur R, Mishra AK and Misra A: Intranasal delivery of cyclobenzaprine hydrochloride-loaded thiolated chitosan nanoparticles for pain relief. Journal of drug targeting 2013; 21(8): 759-69.
22.    Pathan SA, Iqbal Z, Zaidi S, Talegaonkar S, Vohra D, Jain GK, Azeem A, Jain N, Lalani JR, Khar RK and Ahmad FJ: CNS drug delivery systems: novel approaches. Recent patents on drug delivery & formulation 2009; 3(1): 71-89.
23.    Begley DJ: Delivery of therapeutic agents to the central nervous system: the problems and the possibilities. Pharmacology and Therapeutics 2004; 104(1): 29-45.
24.    More BA, Mene HR, Pawar RK, Misal NS, Pathak SS and Shivshara KJ: A review on in-situ nasal gel drug delivery system. Int J Pharm Sci Rev Res 2015; 33: 199-207.
25.    Singh S, Kanupriya H and Kumar H: Intranasal thermo reversible mucoadhesive gels: a review. Int J Pharm 2012; 2(3): 548-56.
26.    Remeth J, Kailas K, Jitendra VS, Havaldar VD and Rahul K: Formulation and evaluation of thermoreversible mucoadhesive nasal gels of metoclopramide hydrochloride. Latin American Journal of Pharmacy 2010; 29(3): 354-61.
27.    Kumar MV, Aravindram AS, Rohitash K, Gowda DV and Parjanya K: Formulation and evaluation of in-situ gel of bromhexine hydrochloride for nasal delivery. Pharm Sin 2012; 3: 699-707.
28.    Dudhipala N, Narala A and Bomma R: Recent updates in the formulation strategies to enhance the bioavailability of drugs administered via intranasal route. JBB, An Open Access Journal 2016; 8(5): 204-207.
29.    De A, Chakraborty S, Mukherjee A and Chattopadhyay J: Formulation of the in-situ forming mucoadhesive nasal gel of salbutamol using pluronic f-127 as thermosensative gel forming polymer. International Journal of Research in Pharmaceutical and Biomedical Sciences 2013; 4(3): 926-33.
30.    Sharwaree H, Priyanka B, Ashok B and Swapnil M: Development of mucoadhesive nasal in-situ gel to sustain the release of amitriptyline hydrochloride. Int J Biol Pharm Res 2012; 3: 980-9.
31.    Athare AB, Rohamare P, Bansode A, Mahale N and Chaudhari S: Formulation and evaluation of eletriptan hydrobromide thermoreversibal nasal in-situ gel. Int J Pharmaceutical Rech Development 2012; 4(04): 267-75.
32.    Uttarwar S: Formulation and development of in-situ gelling system for nasal administration for an antiemetic drug ondansetron hydrochloride by using Pluronics 127P and Pluronics 68. Int J Res Pharm Biomed Sci 2012; 3: 1103-8.
33.    Bhandwalkar MJ and Avachat AM: Thermoreversible nasal in-situ gel of venlafaxine hydrochloride: formulation, characterization, and pharmacodynamic evaluation. AAPS Pharmscitech 2013; 14(1): 101-10.

Recomonded Articles:

Author(s): Dipti G. Phadtare, Amol R. Pawar, R.B. Saudagar, Govind K.Patil

DOI: 10.5958/0975-4377.2017.00002.7         Access: Open Access Read More

Author(s): Swapnil T. Deshpande, P. S. Vishwe, Rohit D. Shah, Swati S. Korabu, Bhakti R. Chorghe, DG Baheti

DOI:         Access: Open Access Read More

Author(s): Chirag A. Patel, Priyal R. Patel, Dhrubo Jyoti Sen,Jayvadan K. Patel

DOI:         Access: Open Access Read More

Author(s): Patil Namrata D., Gondkar S.B., Saudagar R.B.

DOI: 10.5958/0975-4377.2016.00033.1         Access: Open Access Read More

Author(s): Hardik B. Rana, Kajol Patel, Mansi Dholakia, Vaishali T. Thakkar, Mukesh C. Gohel, Tejal R. Gandhi

DOI: 10.5958/0975-4377.2017.00006.4         Access: Open Access Read More

Author(s): Debjit Bhowmik, Amrendra Singh , Praveen Khirwadkar, Nishi Shukla, Vikas Kumar Chaudhari

DOI: 10.5958/0975-4377.2016.00027.6         Access: Open Access Read More

Author(s): Masheer Ahmed Khan

DOI:         Access: Open Access Read More

Author(s): Kritika Kanoujia, Chandraprabha Dewangan, Ayushi Masih, Dipti Sinha, Divya Oraon, Manisha Jaiswal, Monika Sahu, Ranjeeta Kumari, Sapna Pradhan, Ravi Suman, Rajkishan Dewangan, Roman Banjare, Pradeep Paikra, Mukesh Rawtiya, Mukta Agrawal, Ajazuddin, D. K. Tripathi, Amit Alexander

DOI: 10.5958/0975-4377.2018.00015.0         Access: Open Access Read More

Author(s): Swati Rawat, Shradha Sangali, Akhilesh Gupta

DOI: 10.5958/0975-4377.2018.00001.0         Access: Open Access Read More

Author(s): Nakkala Balaji , V. Sai Kishore , Kasani Hari Krishna Gouda

DOI:         Access: Open Access Read More

Author(s): Shoaib Ahmad

DOI: 10.5958/0975-4377.2016.00041.0         Access: Open Access Read More

Author(s): V. Saikishore, G. Srikanth, Ch. Pooja, Y. Mrudula, R. Pavani, Ch. Jyosthna , C. Mayuren

DOI:         Access: Open Access Read More

Author(s): Suresh A. Marnoor

DOI:         Access: Open Access Read More

Author(s): Amit K. Jain, Rajput Rammulrajsinh, Pradeep Agrawal, Kinal patel

DOI:         Access: Open Access Read More

Author(s): Patel Chirag J., Asija Sangeeta, Patel Pinkesh, Mangukia Dhruv, Satyanand Tyagi

DOI:         Access: Open Access Read More

Author(s): Varsha R. Sandhan, S.B. Gondkar, R. B. Saudagar

DOI:         Access: Open Access Read More

Research Journal of Pharmaceutical Dosage Forms and Technology (RJPDFT) is an international, peer-reviewed journal, devoted to pharmaceutical sciences. ...... Read more >>>

RNI: Not Available                     
DOI: 10.5958/0975-4377 


Recent Articles




Tags