Swarupa Arvapalli, A. Anka Rao
Swarupa Arvapalli1*, A. Anka Rao2
1Research Scholar, College of Pharmacy, Koneru Lakshmaiah Education Foundation, Vaddeswaram, Andhra Pradesh. 522502.
2Associate Professor, College of Pharmacy, Koneru Lakshmaiah Education Foundation, Vaddeswaram, Andhra Pradesh. 522502.
Volume - 16,
Issue - 2,
Year - 2023
This research work focuses on development of proniosomal efavirenz (EFV) formulation using maltodextrin as a carrier. Thus an effort is made to increase the effectiveness of oral drug delivery of EFV by blending them in proniosomal powders (maltodextrin-based). The slurry method was employed for the preparation of proniosomes. A mix of Span-60, cholesterol and maltodextrin were used for its preparation..Box Behnken Design used to study the effect of independent variables X1, X2, and X3 (maltodextrin, Span-60 and cholesterol) on response variables Y1, Y2 and Y3 (Entrapment efficiency ,Vesicle size and Cumulative Drug Release percentage). Scanning Optical electron microscopy was used for studying surface-morphology of proniosome (optimized) and proniosome formation. To study any drug interaction or its conversion to the molecular and amorphous state from crystalline state, various tests like differential scanning calorimetry and FT-IR were performed. Compared to EFV in pure form, the proniosomalmaltodextrinbaseddrug showed better dissolution 98.41% in vitro-dissolution study. The optimized Efavirenz loaded proniosomal formulation showed maximum permeation (2614±215µg) in rat intestine as compared to pure drug(1500±114µg). The effectiveness of this drug (oral delivery) is obvious from the fact that rat intestine drug permeation is better. This shows maltodextrin-based EVF proniosomal formulation is suitable for oral delivery of efavirenz.
Cite this article:
Swarupa Arvapalli, A. Anka Rao. Preparation, Characterization and Optimization of Maltodextrin based Efavirenz loaded Proniosomes using Box Behnken Design: In vitro and ex-vivo permeation study. Research Journal of Pharmacy and Technology 2023; 16(2):669-5. doi: 10.52711/0974-360X.2023.00114
Swarupa Arvapalli, A. Anka Rao. Preparation, Characterization and Optimization of Maltodextrin based Efavirenz loaded Proniosomes using Box Behnken Design: In vitro and ex-vivo permeation study. Research Journal of Pharmacy and Technology 2023; 16(2):669-5. doi: 10.52711/0974-360X.2023.00114 Available on: https://rjptonline.org/AbstractView.aspx?PID=2023-16-2-33
1. Singh, P., Verma, A., Mittal, P. and Khinchi, M.P., 2013. Self Emulsifying Drug Delivery System: An Approach To Enhance Oral Bioavailability. Asian Journal of Pharmaceutical Research and Development, pp.178-193.
2. Figueroa-Campos, A., Sánchez-Dengra, B., Merino, V., Dahan, A., González-Álvarez, I., García-Arieta, A., González-Álvarez, M. and Bermejo, M., 2020. Candesartan cilexetil in vitro–in vivo correlation: predictive dissolution as a development tool. Pharmaceutics, 12(7), p.633.https://doi.org/10.3390/pharmaceutics12070633
3. Babadi, D., Dadashzadeh, S., Osouli, M., Abbasian, Z., Daryabari, M.S., Sadrai, S. and Haeri, A., 2021. Biopharmaceutical and pharmacokinetic aspects of nanocarrier-mediated oral delivery of poorly soluble drugs. Journal of Drug Delivery Science and Technology, 62, p.102324.https://doi.org/10.1016/j.jddst.2021.102324
4. Ahad, A., Raish, M., Al-Jenoobi, F.I. and Al-Mohizea, A.M., 2018. Sorbitane monostearate and cholesterol based niosomes for oral delivery of telmisartan. Current drug delivery, 15(2), pp.260-266. https://doi.org/10.2174/1567201814666170518131934
5. Baig, M.R., Shahiwala, A. and Khan, S.A., 2018. Sensible Use of Technologies to Increase Solubility and Bioavailability in Formulation Development. Advancements in Bioequivalence & Bioavailability, 1(1), pp.1-4.
6. Mohanty, D., Rani, M.J., Haque, M.A., Bakshi, V., Jahangir, M.A., Imam, S.S. and Gilani, S.J., 2020. Preparation and evaluation of transdermal naproxen niosomes: formulation optimization to preclinical anti-inflammatory assessment on murine model. Journal of liposome research, 30(4), pp.377-387.
7. Jangam, R.P., Thombre, A.N. and Gaikwad, N.P., 2017. A review: proniosomes as a novel drug delivery system. Asian Journal of Pharmacy and Technology, 7(3), pp.166-174.
8. Debnath, A. and Kumar, A., 2015. Structural and functional significance of niosome and proniosome in drug delivery system. International Journal of Pharmacy and Engineering, 3(3), pp.621-637.
9. Upadhye, S. and Rafik, I.N., 2020. Proniosomes: A novel vesicular drug delivery system. Am. j. PharmTech res, 10(2), pp.260-273.
10. Mogatle, S., 2008. African traditional medicines-antiretroviral drug interactions: the effect of african potato (Hypoxishemerocallidea) on the pharmacokinetics of efavirenz in humans (Doctoral dissertation, Rhodes University)
11. Ganta, K.K., Mandal, A. and Chaubey, B., 2017. Depolarization of mitochondrial membrane potential is the initial event in non-nucleoside reverse transcriptase inhibitor efavirenz induced cytotoxicity. Cell biology and toxicology, 33(1), pp.69-82.https://doi.org/10.1007/s10565-016-9362-9
12. Chiappetta, D.A., Hocht, C., Taira, C. and Sosnik, A., 2010. Efavirenz-loaded polymeric micelles for pediatric anti-HIV pharmacotherapy with significantly higher oral bioavailability. Nanomedicine, 5(1), pp.11-23.https://doi.org/10.2217/nnm.09.90
13. Ismail, S. and Khattab, A., 2018. Optimization of proniosomal itraconazole formulation using Box Behken design to enhance oral bioavailability. Journal of Drug Delivery Science and Technology, 45, pp.142-150.https://doi.org/10.1016/j.jddst.2018.03.013
14. Khudair, N., Agouni, A., Elrayess, M.A., Najlah, M., Younes, H.M. and Elhissi, A., 2020. Letrozole-loaded nonionic surfactant vesicles prepared via a slurry-based proniosome technology: Formulation development and characterization. Journal of Drug Delivery Science and Technology, 58, p.101721.https://doi.org/10.1016/j.jddst.2020.101721
15. Zhou, Y., Li, W., Chen, L., Ma, S., Ping, L. and Yang, Z., 2010. Enhancement of intestinal absorption of akebia saponin D by borneol and probenecid in situ and in vitro. Environmental toxicology and pharmacology, 29(3), pp.229-234.https://doi.org/10.1016/j.etap.2010.01.004
16. Samein, L.H., 2014. Preparation and evaluation of nystatin-loaded solid-lipid-nanoparticles for topical delivery. Asian Journal of Pharmaceutical Research, 4(1), pp.44-51.
17. Sharma, A., Guarve, K. and Singh, R., 2021. Application of Box–Behnken Design and Desirability function in the Optimization of Aceclofenac-Loaded Micropsonges for Topical Application. Research Journal of Pharmacy and Technology, 14(12), pp.6295-6303. DOI: 10.52711/0974-360X.2021.01089
18. Jangam, R.P., Thombre, A.N. and Gaikwad, N.P., 2017. A review: proniosomes as a novel drug delivery system. Asian Journal of Pharmacy and Technology, 7(3), pp.166-174.
19. Raju, T.G., Ramya, M.G., Rajesh, A., Kathirvel, S. and Gupta, S.K., 2014. ICH Guideline Practice-a Validated Stability-Indicating HPLC Method for the Determination of Efavirenz in Dosage Form. Research Journal of Pharmaceutical Dosage Forms and Technology, 6(1), pp.7-14.
20. Sharma, A., Guarve, K. and Singh, R., 2021. Application of Box–Behnken Design and Desirability function in the Optimization of Aceclofenac-Loaded Micropsonges for Topical Application. Research Journal of Pharmacy and Technology, 14(12), pp.6295-6303. DOI: 10.52711/0974-360X.2021.01089
21. Kaushal, A., Arora, S., Singh, S. and Sharma, N., 2020. Assessing the impact of formulation variables on dissolution profile of sustained release tablet of metformin hydrochloride by quality by design approach. Research Journal of Pharmacy and Technology, 13(5), pp.2350-2358.