ANTIEPILEPTIC RECTAL HYDROGEL LOADED WITH CARBAMAZEPINE – RICE BRAN WAX MICROSPHERES

  • Sreeja C Nair LECTURER,DEPARTMENT OF PHARMACEUTICS, AMRITA SCHOOL OF PHARMACY,AMRITA VISHWAVIDYAPEETHAM UNIVERSITY, AIMS- PONEKKARA P.O, KOCHI, KERALA, INDIA.
  • Krishnapriya M
  • Karthika Ramesh

Abstract

ABSTRACT
Objectives: The objective behind the study is to develop a mucoadhesive rectal hydrogel from carbamazepine (CBZ) – rice bran wax (RBW)
microspheres for the purpose of controlled release for the treatment of epilepsy.
Methods: The study was conducted to formulate controlled release rectal hydrogel loaded with CBZ – RBW microspheres in two different natural polymers,
RBW and collagen which are prepared by modified cooling induced solidification method and gel preparation along with their evaluation studies.
Results: A thorough analysis of the optimized gel revealed that all the evaluation parameters evaluated are within the acceptable limits. Further, the
optimized microsphere formulation (M5) was used to formulate it as rectal hydrogel using polymer collagen and was characterized. The mucoadhesion
time of 25% w/w collagen hydrogel (H4) was 565 minutes, allowing the loaded microspheres to be attached on rectal mucosa. In vitro drug release
from the mucoadhesive hydrogel formulations showed controlled drug release pattern with a maximum drug release of 96.45±0.35% for optimized
H4 formulation after 12 hr, followed zero order release pattern with diffusion mediated Higuchi model. Ex vivo permeation studies using bovine rectal
mucosa revealed that H4 formulation showed greater permeability compared to control. Histopathological findings revealed that H4 formulation is
safer for rectal administration without any signs of rectal irritancy. The stability studies of optimized formulation (H4) proved that hydrogel remained
stable over a wide range of temperature condition.
Conclusion: Hence, the developed rectal hydrogel formulation seems to be a viable alternative to conventional drug delivery system for the effective
management of epilepsy.
Keywords: Carbamazepine, Rice bran wax, Rectal hydrogel, Sustainability.

Author Biography

Sreeja C Nair, LECTURER,DEPARTMENT OF PHARMACEUTICS, AMRITA SCHOOL OF PHARMACY,AMRITA VISHWAVIDYAPEETHAM UNIVERSITY, AIMS- PONEKKARA P.O, KOCHI, KERALA, INDIA.
DEPARTMENT OF PHARMACEUTICS

References

REFERENCES
1. Wallace H, Shorvon S, Tallis R. 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 1998;352(9145):1970-3.
2. Engelborghs S, D’Hooge R, De Deyn PP. Pathophysiology of epilepsy. Acta Neurol Belg 2000;100(4):201-13.
3. Ramesh K, Krishnapriya M, Anupriya, Nair SC. An outlook to non-pharmacological and novel approaches to combat the uncurable firing disorder. Int J Pharm Sci Rev Res 2016;40(1):55-61.
4. Nair SC, Anoop KR. Local antimicrobial delivery of satranidazole loaded cross linked periodontal chips using bio degradable polymers. Int J Pharm Pharm Sci 2013;5(3):839-47.
5. Prasanth VV, Moy AC, Mathew ST, Mathapan R. Microspheres-an
Fig. 10: Ex vivo permeation comparison studies of selected formulations with control
Fig. 12: Scanning electron microscopy of carbamazepine rice bran wax microsphere loaded hydrogel (H4 formulation)
Fig. 13: Stability study of optimized rectal hydrogel (H4)
Fig. 11: (a-c) Histopathological evaluation
a
b
c
270
Asian J Pharm Clin Res, Vol 10, Issue 3, 2017, 264-270
Krishnapriya et al.
overview. Int J Pharm Biomed Sci 2011;2(2):332-8.
6. Vashist A, Ahmad S. Hydrogels: Smart materials for drug delivery. Orient J Chem 2013;29(3):861-70.
7. Cloyd JC, Lalonde RL, Beniak TE, Novack GD. A single-blind, crossover comparison of the pharmacokinetics and cognitive effects of a new diazepam rectal gel with intravenous diazepam. Epilepsia 1998;39(5):520-6.
8. Sahil K, Akanksha M, Premjeet S, Bilandi A, Kapoor B. Microsphere: A review. Int J Res Pharm Chem 2011;1(4):1184-98.
9. Saboktakin MR, Tabatabaie RM, Maharramov A, Ramazanov MA. Synthesis and characterization of biodegradable chitosan beads as nano-carriers for local delivery of satranidazole. Carbohydr Polym 2010;81(3):726-31.
10. Jain SK, Jain A, Gupta Y, Ahirwar M. Design and development of hydrogel beads for targeted drug delivery to the colon. AAPS PharmSciTech 2007;8(3):E56.
11. Fahim F, Naseer A, Ahmed S, Sherazi ST, Bhanger MI. A green approach for the determination of selected anti-diabetic drugs in pharmaceutical formulation by transmission FTIR spectroscopy. J Braz Chem Soc 2014;25(11):2032-8.
12. Ishaka A, Umar Imam M, Mahamud R, Zuki AB, Maznah I. Characterization of rice bran wax policosanol and its nanoemulsion formulation. Int J Nanomedicine 2014;9:2261-9.
13. Ibrahim MM, Sammour OA, Hammad MA, Megrab NA. In vitro evaluation of proniosomes as a drug carrier for flurbiprofen. AAPS PharmSciTech 2008;9(3):782-90.
14. Choi HG, Jung JH, Ryu JM, Yoon SJ, Oh YK, Kim CK. Development of in situ-gelling and mucoadhesive acetaminophen liquid suppository. Int J Pharm 1998;165(1):33-44s.
15. El-Samaligy MS, Yahia SA, Basalious EB. Formulation and evaluation of diclofenac sodium buccoadhesive discs. Int J Pharm 2004;286(1-2):27-39.
16. El-Hady SA, Mortada ND, Awad GA, Zaki NM, Taha RA. Development of in situ gelling and mucoadhesive mebeverine hydrochloride solution for rectal administration. Saudi Pharm J 2003;11(4):159-71.
17. Dragicevic-Curic N, Scheglmann D, Albrecht V, Fahr A. Temoporfin-loaded invasomes: Development, characterization and in vitro skin penetration studies. J Control Release 2008;127(1):59-69.
18. El-Leithy ES, Shaker DS, Ghorab MK, Abdel-Rashid RS. Evaluation of mucoadhesive hydrogels loaded with diclofenac sodium-chitosan microspheres for rectal administration. AAPS PharmSciTech 2010;11(4):1695-702.
19. Shivhareu D, Tijare PM. Formulationand characterization of microspheres of selected anti-infective agent for urinary tract infection. J Drug Dev Res 2013;2(1):16-26.
20. John MS, Nair SC, Anoop KR. Thermoreversible mucoadhesive gel for nasal delivery of anti hypertensive drug. Int J Pharm Sci Rev Res 2013;21(1):57-63.
21. Nair RV, Nair SC. Cross linked chitosan in situ gel of satranidazole for intra periodontal drug delivery. Int Res J Pharm 2014;5(4):239-43.
22. Nair AS, Vidhya KM, Saranya TR, Sreelakshmy KR, Nair SC. Mucoadhesive buccal patch of cefixime trihydrate using biodegradable natural polymer. Int J Pharm Pharm Sci 2014;6(6):366-71.
Statistics
317 Views | 323 Downloads
How to Cite
Nair, S., K. M, and K. Ramesh. “ANTIEPILEPTIC RECTAL HYDROGEL LOADED WITH CARBAMAZEPINE – RICE BRAN WAX MICROSPHERES”. Asian Journal of Pharmaceutical and Clinical Research, Vol. 10, no. 3, Mar. 2017, pp. 264-70, doi:10.22159/ajpcr.2017.v10i3.16144.
Section
Original Article(s)