Design And Development Of Mucoadhesive Microspheres Of Chlorpheniramine Maleate For Nasal Delivery

Authors

  • Riya Pathak
  • Jaideo Pandey

Keywords:

Nasal Delivery, Mucoadhesion, Microsphere, Chlorpheniramine maleate, Chitosan, Emulsification-cross linking

Abstract

Drug delivery methods that allow for prolonged, close contact between the drug and the mucosa are known as mucoadhesive drug delivery systems. In order to prevent hepatic first-pass metabolism, increase residence time, and improve therapeutic efficacy, the current study aimed to produce mucoadhesive microspheres for nasal delivery. In our work, we used the Emulsification cross linking approach to create Chlorpheniramine maleate mucoadhesive microspheres with conjugation of chitosan. The microspheres were assessed in terms of their stability, in vitro drug release, in vitro mucoadhesion, percentage yield, particle size, entrapment efficiency, and swelling properties. Using SEM and FTIR technologies, microspheres were characterised. Each batch's average microsphere’s particle size was found compiling with in the desired/recommended range, ensuring that every batch had appropriate handling qualities. It was discovered that the range of drug encapsulation efficiency, percentage yield & percentage for mucoadhesion for all formulations were observed to justify the recommended range. When all of the formulations were tested for In-vitro drug release using phosphate buffer 6.8 pH, microspheres showed regulated drug release for up to six hours. According to the results gathered, mucoadhesive microsphere technology represents a very promising nasal delivery for improving patient compliance and delivering medication over an extended period of time

Downloads

Download data is not yet available.

Metrics

Metrics Loading ...

References

Adimoodlam S, Chavda GA, Patel JN, Jimson J, and Narayana SVB: Formualation and Evaluation of Tinazidine Hydrochloride Microspheres by using 32 Full Factorial Designs. Internation research journal of pharmacy.2011; 2 (9):110-115.

Al-Helw AA, Al-Angary AA, Mahrous GM, Al-Dardari MM: Preparation and Evaluation of Sustained Release Cross-linked Chitosan Microspheres Containing Phenobarbitone. Journal of Microencapsulation. 1998; 15: 373– 382

Ali, Huma, Muhammad Harris Shoaib, and Rabia Bushra. "Formulation development of pheniramine maleate tablet by direct compression." Jordan Journal of Pharmaceutical Sciences 4.1 (2011): 1-8.

Bhoi, Ganesh S., et al. "Formulation and evaluation of medicated chewing gum containing chlorpheniramine maleate." Indo Am J Pharm Res 4.3 (2014): 1309-1319.

Callens, Catherine, and Jean Paul Remon. "Evaluation of starch–maltodextrin–Carbopol® 974 P mixtures for the nasal delivery of insulin in rabbits." Journal of controlled release 66.2-3 (2000): 215-220.

Chintagunta P, Kavitha K and Anil KSN: Formulation and Evaluation of Trimetazidine Hydrochloride Loaded Chitosan Microspheres. International Journal of Applied Pharmaceutics. 2010; 2; 11-14.

Chowdary KPR, and Rao YS: Mucoadhesive Microspheres and Micro Capsules: Current Status. Indian Journal of Pharmaceutical Sciences. 2005; 67(2):141-150.

Desai S, Gali Vidyasagar G, Shah V, Desai D: Preparation and in vitro Characterization of Mucoadhesive Microspheres of Midazolam: Nose to Brain Administration, Asian Journal of Pharmaceutical and Clinical Research. 2011; 4: 100-102.

Deshmukh T, Deshmukh V, Jadhav P, Kasat K and Patil R: Formulation and Evaluation of Mucoadhesive Microspheres of Ziprasidone Hydrochloride for Oral Controlled Release. Journal of Current Pharma Research, 2012; 497- 502.

Gavini E and Hegg AB: Nasal Administration of Carbamazepine using Chitosan Microspheres in-vitro / in-vivo studies. International Journal of Pharmceutical Science. I, 2006; 307: 9-15.

Gavini E, Rassu G, Sanna V, Cossu M and Giunchedi P: Mucoadhesive Microsphere for Nasal Administration of an Antiemetic Drug, Metoclopramide: In-vitro/Ex-vivo Studies. Journal of Pharmacy and Pharmacology. 2005; 57: 287-294

Ghosh PK: Thernoreversible- Mucoadhesive Gel for Nasal Delivery of Sumatriptan. AAPS Pharm Sci Tech, 2006; 7: 100-102.

Hardenia SS, Jain A, Patel R and Kaushal A: Formulation and Evaluation of Mucoadhesive Microspheres of Ciprofloxacin. Journal of Advanced Pharmacy Education and Research. 2011; 214-222.

Jadhav KR, Gambhire MN, Shaikh IM, Kadam VJ and Pisal SS: Nasal Drug Delivery System-Factor Affecting and Applications. Current Drug Therapy, 2007; 27-38.

Jameela SR, Kumary TV, Lal AV and Jayakrishnan A: Progesterone-Loaded Chitosan Microspheres: A Long Acting Biodegradable Controlled Delivery System. Journal of Controlled Release. 1998; 52: 17–24.

Jain AJ, Chauk DS, Mahajan HS, Tekade AR and Gattani SG: Formulation and Evaluation of Nasal Mucoadhesive Microspheres of Sumatriptan Succinate. Journal of Microencapsulation, 2009; 26(8): 711–721.

Kavita K and Rajas NJ: Sustained Opthalmic Delivery of Levofloxacin Hemihydrate from an Ion Activated In-situ Delling System. International Journal of PharmTech Research 3, 2011; 702-706.

Krishnamoorthy R and Mitra AK: Prodrugs for Nasal Drug Delivery. Advanced Drug Delivery Rev 29, 1998; 135-46.

Kumar, Manish, et al. "Chlorpheniramine maleate containing chitosan-based nanoparticle-loaded thermosensitive in situ gel for management in allergic rhinitis." Drug Delivery and Translational Research 9.6 (2019): 1017-1026.

Mahajan H, Gattani S and Surana S: Spray Dried Mucoadhesive Microspheres of Ondansetron for Nasal Administration. International Journal of Pharmaceutical Sciences and Nanotechnology, 1 2008; 267-274.

Mahalaxmi R and Kumar S: Preparation of Mucoadhesive Microspheres for Nasal Delivery by Spray Drying. Indian Journal of Pharmaceutical Sciences, 2007; 9: 651–657.

Mahmood, Sura Zuhair, et al. "Optimization and evaluation of chlorpheniramine maleate oral strip for pediatric use." Optimization 11.12 (2018).

Mainardes RM, Cocenza urban MC, Cinto PO, Chaud MV and Evangelista RC: Liposomes and Micro / Nanoparticles as Colloidal Carriers for Nasal Drug Delivery. Current Drug Delivery 3, 2006; 275-85.

Martin A, Bustamante P, Chun AH and Eds: Physical Pharmacy, 4th Edn, B.J. Waverly Pvt. Ltd; New Delhi, 1996; 423-432.

Martinac A and Pavelic A: Spray Dried Chitosan / Ethyl Cellulose Microspheres for Nasal Drug Delivery: Swelling Study and Evaluation of in vitro Drug Release Properties. Journal of Microencapsulation, 2005, 5: 549-561.

Merkus, F. W. H. M., et al. "Cyclodextrins in nasal drug delivery." Advanced drug delivery reviews 36.1 (1999): 41-57.

Mishra S, Patel NS, Kumar M and Pathak K: Cross-linked Mucoadhesive Microspheres Based on Anionic Eteropolysaccharide for Nasal Delivery of Felodipine: Optimization and in-vitro Evaluation. Drug Delivery Letters. 2013; 3, 136-148.

Pandey JD & Tripathi P, Formulation and Evaluation of Levocetrizine Loaded Mucoadhesive Microspheres for Nasal Delivery. International Journal of Pharmaceutical Sciences and Research (IJPSR) (2016), vol 7, Issue 5, 2242-2251.

Pandey JD & Tripathi P, Mucoadhesive Microspheres of Anti-allergic Agent for Nasal Delivery. Asian Journal of Pharmaceutical Technology and Innovation (2016), vol 4, Issue 18, 48-58.

Patel D, Patel N, Thakkar V, Modi A and Gandhi T: Development and Characterization of Mucoadhesive Microspheres of Levosalbutamol Sulphate. International Journal of Pharmaceutical Sciences and Research. 2013; 4(5): 1838-1851.

Patel, AMIT A., Rajesh H. Parikh, and Tejal A. Mehta. "Development optimization and evaluation of effervescent tablets of chlorpheniramine maleate using Box Behnken design." Int J Pharm Pharm Sci 7.8 (2015): 317-23.

Patil SB & Sawant K: Chitosan Microspheres as a Delivery System for Nasal Insufflations. Colloids and Surfaces, Biointerfaces. 2011; 84; 384–389.

Prajapati RK, Mahajan HS and Surana SJ: PLGA Based Mucoadhesive Microspheres for Nasal Delivery: In vitro/Ex vivo Studies. Indian Journal of Novel Drug Delivery. 2011; 3 (1):9-16.

Rajalakshmi AN and Bhuwaneshwari B: Short Review on Pharmaceutical Microspheres: Interantional Journal of Universal Pharmacy and Life Sciences. 2012; 2(2): 2449- 6793.

Ramachandran S, Nandhakumar S and Dhanaraju MD: Formualtion and Characterization of Glutaraldehyde Cross Linked Chitosan Biodegradable Microspheres Loaded with Famotidine. Tropical Journal of Pharmaceutical Research. 2011; 10(3): 309-316.

Rao JV, Gangadi JR, Kumar SM, Venu K and Rao KNV: Formulation and Evaluation of Mucoadhesive Microspheres for Intra-nasal Delivery. International Journal of Pharmacy & Technology. 2010; 2(4): 1158-1198.

Rathan M, Kumar DS, Shirwaikar A, Ravi Kumar D, Sampath Kumar and Prasad RS: Preparation of Mucoadhesive Microspheres for Nasal Delivery by Spray Drying. Indian Journal of Pharmaceutical Sciences , 2007; 69: 651-657.

Sanchez-Gonzalez, Marcos, et al. "A randomized controlled pilot trial to test the efficacy of intranasal chlorpheniramine maleate with xylitol for the treatment of allergic rhinitis." Cureus 13.3 (2021).

Shwetha, S., K. Kamath, and S. K. Kumar. Design and evaluation of floating microspheres of Rabeprazole sodium. International Journal of Pharmacy and Pharmaceutical Sciences 4.3 (2012): 104-120.

Sinha VR, Singla AK, Wadhwan S, Kaushik R, Kumaria R, Basal K, and Dhawan S: Chitosan Microspheres as a Potential Carrier for Drugs. International Journal of Pharmaceutics. 2004; 274: 1-33.

Soane RJ, Frier M, Perkins AC, Jones NS and David SS: Evaluation of the Clearance Characteristics of Bio adhesive System in Human. international Journal of Pharmaceutics. 1999; 178: 55-65

Soliman, Iman I., Nadia A. Soliman, and Ebtsam M. Abdou. "Formulation and stability study of chlorpheniramine maleate nasal gel." Pharmaceutical Development and Technology 15.5 (2010): 484-491.

Swamy NGN and Abbas Z: Preparation and In-vitro Characterization of Mucoadhesive Polyvinyl Alcohol Microspheres Containing Amlodipine Besylate for Nasal Administration. Indian Journal of Pharmaceutical Education and Research. 2012; 46: 52-58.

Taş, Çetin, et al. In vitro and ex vivo permeation studies of chlorpheniramine maleate gels prepared by carbomer derivatives. Drug development and industrial pharmacy 30.6 (2004): 637-647.

Tatiya GD and Basarkar GD: Formulation Development and In-vitro Evaluation of Mucoadhesive Microspheres of Simvastatin for Nasal Delivery. International Journal of Pharmaceutical Sciences Review and Research. 2013; 21(2): 334-341.

Thanoo BC, Sunny MC and Jayakrishnan A: Cross-linked Chitosan Microspheres: Preparation and Evaluation as a Matrix for the Controlled Release of Pharmaceuticals. Journal of Pharmacy and Pharmacololgy. 1992; 44: 283– 286

Ugwoke M, Agu R, Verbeke N, and Kinget R: Nasal Mucoadhesive Drug Delivery: Background, Applications, Trends and Future Perspectives. Advance Drug Delivery Review.2005; 57: 1640–1665.

Ugwoke, Michael Ikechukwu, et al. Intranasal bioavailability of apomorphine from carboxymethylcellulose-based drug delivery systems. International journal of pharmaceutics 202.1-2 (2000): 125-131.

Viswanadhan Vasantha, Prasanth, et al. "Combination of cellulose derivatives and chitosan-based polymers to investigate the effect of permeation enhancers added to in situ nasal gels for the controlled release of loratadine and chlorpheniramine." Polymers 15.5 (2023): 1206.

Wamorkar V, Manjunath SY and Verma MM: Development and Validation of UV Spectroscopic Method for Determination of Metoclopramide Hydrochloride in Bulk and Tablet Formulation. International Journal of Pharmacy and Pharmaceutical Sciences. 2011; 3(3); 171-174.

Yetkin, G., et al. "The effect of dimethyl-beta-cyclodextrin and sodium taurocholate on the nasal bioavailability of salmon calcitonin in rabbits." STP pharma sciences, 1999; 9(3): 249-252.

Yuvraj S, Dangi, and Kamta PN: Preparation, Optimization and Characterization of Controlled Release Mucoadhesive Microspheres Containing Highly Variable Drug Itraconazole in Reducing Gastric Variability as Compared to Innovator Formulation. Scholar Research Library. 2010: 37-51.

Zuheir A, Samein LH and Alash N: Preparation and In-vitro Evaluation of Metoclopramide HCL Hollow-Type Suppository. International Journal of Pharmacy and Pharmaceutical Sciences. 2013, 660-666.

Downloads

Published

2025-08-13

How to Cite

1.
Pathak R, Pandey J. Design And Development Of Mucoadhesive Microspheres Of Chlorpheniramine Maleate For Nasal Delivery. J Neonatal Surg [Internet]. 2025Aug.13 [cited 2025Nov.1];14(15S):2446-5. Available from: https://www.jneonatalsurg.com/index.php/jns/article/view/8873