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Rektal ilaç dağıtımı için karbopol içeren mukoadhezif termo-ters çevrilebilir sukralfat jellerinin formülasyonunun geliştirilmesi ve değerlendirilmesi

Year 2021, Volume: 41 Issue: 4, 234 - 242, 01.12.2021
https://doi.org/10.52794/hujpharm.1012883

Abstract

References

  • 1. Gonjari ID, Hosmani AH, Karmarkar AB, Godage AS, Kadam SB, Dhabale PN, et al: Formulation and evaluation of in situ gelling thermoreversible mucoadhesive gel of fluconazole. Drug Discov Ther, 3, 6-9 (2009).
  • 2. Sheeba JM, Sreeja C, Anoop KR : Thermo reversible mucoadhesive gel for nasal delivery of antihypertensive drug. Int J Pharm Sci Rev Res, 21, 57-63 (2013).
  • 3. Elhady A, Seham S, Naheed DM, Gehanne AS, Noha MZ. : Development of in situ gelling and mucoadhesive mebeverine hydrochloride solution for rectal administration. Saudi Pharm J, 11, 8 (2003).
  • 4. 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, 11, 1695-702 (2010).
  • 5. Anmol C, Rajdeep S, Agarwal PN. : Management of hemorrhoids. Ind JClin Pract, 25, 577-80 (2014).
  • 6. Rahimi R, Abdollahi M.: A systemic review of the topical drugs for post hemorrhoidectomy pain. Int J Pharmacol, 8, 628-637 (2012).
  • 7. Kudaravalli P, John S. Sucralfate. [Updated 2021 Jul 19]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2021 Jan - Available from: https://www.ncbi.nlm.nih.gov/ books/NBK551527/
  • 8. Ala S, Saeedi M, Eshghi F Rafati M, Hejazi V, Hadianamrei R. : Efficacy of 10% sucralfate ointment in the reduction of acute postoperative pain after open hemorrhoidectomy: a prospective double-blind, randomized, placebo-controlled trial. World J Surg, 37(1), 233-238 (2013).
  • 9. Gupta PJ, Heda PS, Kalaskar S, Tamaskar VP. : Topical sucralfate decreases pain after hemorrhoidectomy and improves healing: a randomized, blinded, controlled study. Dis Colon Rectum, 51(2), 231-234 (2008).
  • 10. Nahla S.Barakat.: In vitro and In vivo characteristics of a Thermogelling rectal Delivery system of Etodolac. AAPS Pharm Sci Tech., 10(3), 724 (2009).
  • 11. Cho HJ, Balakrishnan P, Park EK, Song KW, Hong SS, Jang TY, et al. : Poloxamer/cyclodextrin/chitosan-based thermoreversible gel for intranasal delivery of fexofenadine hydrochloride. J Pharm Sci, 100, 681-91 (2011).
  • 12. Prabhakar AN, Mallapa DP, Panchaxari GA, Paresh M. : Formulation and characterization of tapentadol loaded emulgel for topical application. Ind J Pharm Educ Res, 51, 525-35 (2017).
  • 13. Joshu AJ, Kumar AA, Verjina CU, Vasudevan DT, Saritha A. : Formulation and evaluation of antiaging phytosomal gel. Asiam J Pharm Clin Res, 3, 409-22 (2018).
  • 14. Patil PR, Salve VK, Thorat U, Shahi SR. : Formulation and evaluation of ion-sensitive in-Situ nasal gel of zolmitriptan. Int J Pharm Pharm Sci, 7, 47886 (2015).
  • 15. Meenakshi P, Thakkar H, Kasture PV. : Preparation and evaluation of thermoreversible formulations of flunarizine hydrochloride for nasal delivery. Int J Pharm Pharm Sci, 2, 116-20 (2010).
  • 16. Bagul U, Gujar K, Dhat S, Aphale S, Bhavsar M. : In vitro study of mucoadhesive strength of polymers for mucoadhesive drug delivery systems. Int J Curr Pharm Res, 1, 42-6 (2009).
  • 17. Bhupen K, Kritika S, Bansmita K : Development and characterization of mucoadhesive microsphere loaded intranasal gel of venlafaxine HCl. Asian J Pharm Clin Res, 3 Suppl 9, 139-44 (2016).
  • 18. Umme H, Shivakumar HG. : Development of miconazole nitrate thermo sensitive bioadhesive vaginal gel for vaginal candidiasis. Am J Adv Drug Deliv, 1, 358-68 (2013).
  • 19. Contreras MD, Sanchez R.: Application of a factorial design to the study of the flow behavior, spreadability and transparency of a carbopol ETD 2020 gel. Int J Pharm, 234, 149-57 (2002).
  • 20. Firoz S, Padmini K, et al.: Formulation development and evaluation of carbopol-incorporated thermoreversible gels of pseudoephedrine for rectal drug delivery. Asian Journal of Pharmaceutical and Clinical Research, 12(5), 231-5 (2019).

Formulation development and evaluation of carbopol-incorporated mucoadhesive thermoreversible gels of sucralfate for rectal drug delivery

Year 2021, Volume: 41 Issue: 4, 234 - 242, 01.12.2021
https://doi.org/10.52794/hujpharm.1012883

Abstract

Objective : The present study describes the preparation and evaluation of a Poloxamer 188 (P188)-based thermoreversible gel using Carbopol 934P (C934P) as a mucoadhesive polymer of Sucralfate for enhancing the bioavailability and to avoid the first-pass metabolism. Methods: Eight formulations (F1-F8) were prepared using cold method. The prepared gels were characterized by pH, drug content, spreadability, mucoadhesive force, gelation temperature, and drug release profile. Thermoreversibility of P188/C934P gel was demonstrated by rheological studies. The drug-polymer compatibility was studied using Fourier transform infrared (FTIR). The incorporation of carbopol into P188 gel also reduced the amounts of drug released from the gel formulations.
Results: FT-IR studies revealed that there are no interactions between the drug and polymers. Drug content of gels was estimated and the results were found to be satisfactory. In vitro dissolution studies revealed a good drug release from the gels. The drug release was higher in formulations F5 and F6 and lower in F4, F7, and F8 formulations. These findings suggested that developed thermoreversible gels could be used as promising dosage forms to rectal drug delivery for prolonged periods in the management of hemorrhoids.

References

  • 1. Gonjari ID, Hosmani AH, Karmarkar AB, Godage AS, Kadam SB, Dhabale PN, et al: Formulation and evaluation of in situ gelling thermoreversible mucoadhesive gel of fluconazole. Drug Discov Ther, 3, 6-9 (2009).
  • 2. Sheeba JM, Sreeja C, Anoop KR : Thermo reversible mucoadhesive gel for nasal delivery of antihypertensive drug. Int J Pharm Sci Rev Res, 21, 57-63 (2013).
  • 3. Elhady A, Seham S, Naheed DM, Gehanne AS, Noha MZ. : Development of in situ gelling and mucoadhesive mebeverine hydrochloride solution for rectal administration. Saudi Pharm J, 11, 8 (2003).
  • 4. 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, 11, 1695-702 (2010).
  • 5. Anmol C, Rajdeep S, Agarwal PN. : Management of hemorrhoids. Ind JClin Pract, 25, 577-80 (2014).
  • 6. Rahimi R, Abdollahi M.: A systemic review of the topical drugs for post hemorrhoidectomy pain. Int J Pharmacol, 8, 628-637 (2012).
  • 7. Kudaravalli P, John S. Sucralfate. [Updated 2021 Jul 19]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2021 Jan - Available from: https://www.ncbi.nlm.nih.gov/ books/NBK551527/
  • 8. Ala S, Saeedi M, Eshghi F Rafati M, Hejazi V, Hadianamrei R. : Efficacy of 10% sucralfate ointment in the reduction of acute postoperative pain after open hemorrhoidectomy: a prospective double-blind, randomized, placebo-controlled trial. World J Surg, 37(1), 233-238 (2013).
  • 9. Gupta PJ, Heda PS, Kalaskar S, Tamaskar VP. : Topical sucralfate decreases pain after hemorrhoidectomy and improves healing: a randomized, blinded, controlled study. Dis Colon Rectum, 51(2), 231-234 (2008).
  • 10. Nahla S.Barakat.: In vitro and In vivo characteristics of a Thermogelling rectal Delivery system of Etodolac. AAPS Pharm Sci Tech., 10(3), 724 (2009).
  • 11. Cho HJ, Balakrishnan P, Park EK, Song KW, Hong SS, Jang TY, et al. : Poloxamer/cyclodextrin/chitosan-based thermoreversible gel for intranasal delivery of fexofenadine hydrochloride. J Pharm Sci, 100, 681-91 (2011).
  • 12. Prabhakar AN, Mallapa DP, Panchaxari GA, Paresh M. : Formulation and characterization of tapentadol loaded emulgel for topical application. Ind J Pharm Educ Res, 51, 525-35 (2017).
  • 13. Joshu AJ, Kumar AA, Verjina CU, Vasudevan DT, Saritha A. : Formulation and evaluation of antiaging phytosomal gel. Asiam J Pharm Clin Res, 3, 409-22 (2018).
  • 14. Patil PR, Salve VK, Thorat U, Shahi SR. : Formulation and evaluation of ion-sensitive in-Situ nasal gel of zolmitriptan. Int J Pharm Pharm Sci, 7, 47886 (2015).
  • 15. Meenakshi P, Thakkar H, Kasture PV. : Preparation and evaluation of thermoreversible formulations of flunarizine hydrochloride for nasal delivery. Int J Pharm Pharm Sci, 2, 116-20 (2010).
  • 16. Bagul U, Gujar K, Dhat S, Aphale S, Bhavsar M. : In vitro study of mucoadhesive strength of polymers for mucoadhesive drug delivery systems. Int J Curr Pharm Res, 1, 42-6 (2009).
  • 17. Bhupen K, Kritika S, Bansmita K : Development and characterization of mucoadhesive microsphere loaded intranasal gel of venlafaxine HCl. Asian J Pharm Clin Res, 3 Suppl 9, 139-44 (2016).
  • 18. Umme H, Shivakumar HG. : Development of miconazole nitrate thermo sensitive bioadhesive vaginal gel for vaginal candidiasis. Am J Adv Drug Deliv, 1, 358-68 (2013).
  • 19. Contreras MD, Sanchez R.: Application of a factorial design to the study of the flow behavior, spreadability and transparency of a carbopol ETD 2020 gel. Int J Pharm, 234, 149-57 (2002).
  • 20. Firoz S, Padmini K, et al.: Formulation development and evaluation of carbopol-incorporated thermoreversible gels of pseudoephedrine for rectal drug delivery. Asian Journal of Pharmaceutical and Clinical Research, 12(5), 231-5 (2019).
There are 20 citations in total.

Details

Primary Language English
Subjects Pharmacology and Pharmaceutical Sciences
Journal Section Research Articles
Authors

Firoz Shaık

Rajasekaran S This is me

Publication Date December 1, 2021
Acceptance Date December 17, 2021
Published in Issue Year 2021 Volume: 41 Issue: 4

Cite

Vancouver Shaık F, S R. Formulation development and evaluation of carbopol-incorporated mucoadhesive thermoreversible gels of sucralfate for rectal drug delivery. HUJPHARM. 2021;41(4):234-42.