Development and Optimization of Lovastatin-loaded Trans-dermal Proniosomal Gel using Box-Behnken Design
DOI:
https://doi.org/10.37285/ijpsn.2018.11.4.7Abstract
In this study, a proniosome-based transdermal drug delivery system of lovastatin was developed by coacervation phase separation method. On the basis of the pilot trials, a 3-factor, 3-level Box–Behnken design was employed to characterize the effect of Cholesterol, soya lecithin and Tween 80 on dependent variables (particle size, entrapment efficiency, and drug release). TEM analysis of optimized formulation has demonstrated the presence of individual Proniosomes in spherical shape. Lovastatin optimized proniosomal formulation F1 shown better particle size and percentage entrapment efficiency and drug release of 99.49% within 24h in slow and controlled manner when compared with control. Kinetic analysis of drug release profiles showed that the systems predominantly released Lovastatin in a zero-order manner with a strong correlation coefficient (R2= 0.9990). The particle size and Zeta potential of the optimized lovastatin proniosomal gel was found to be 138.82 nm and -11.4 mV respectively. Optimized batch of Proniosomes was used for the preparation of Lovastatin - based proniosomal hydrogel by incorporating hydrated Proniosomes to Carbopol matrix to enhance the stability and viscosity of the system. The enhanced skin permeation for prolonged time may lead to improved efficacy and better patient compliance.
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Keywords:
Lovastatin, Proniosomal gel, Box-Behnken Design, Soya lecithin, TEM
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Published
2018-07-31
How to Cite
1.
C S, P RP. Development and Optimization of Lovastatin-loaded Trans-dermal Proniosomal Gel using Box-Behnken Design. Scopus Indexed [Internet]. 2018 Jul. 31 [cited 2024 May 18];11(4):4196-207. Available from: http://www.ijpsnonline.com/index.php/ijpsn/article/view/382
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Research Articles
References
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Vyas SP and Khar R.K (2004). Targeted and Controlled Drug Delivery-Novel Carrier Systems, first ed., CBS Publishers and Distributors, India: 249-279.
Vora B, Khopade A.J and Jain N.K (1998). Proniosomes based transdermal delivery of levonorgestrel for effective contraception. J Control Rel 54:149-165.
Wen MM, Farid RM and Kaseem AA (2014). Nano-proniosomes enhancing the transdermal delivery of mefenamic acid, J. Liposome Res 24: 280-289.
Yousuf M, Ahmad M, and Usman I Ali (2013). Ketotifen Fumarate and Salbutamol Sulphate Combined Transdermal Patch Formulations: In vitro release and Ex vivo Permeation Studies. Indian J Pharm Sci 75(5): 569-577.
Yasam VR, Jakki SL, Natarajan J, and Kuppusamy G (2014). A review on novel vesicular drug delivery: proniosomes, Drug Deliv 21: 243-249.
Aggarwal G and Dhawan S (2010). Psychotropic drugs and transdermal delivery: an overview, Int. J. Pharm. Bio Sci 1:1-12.
Balch DA and Cooke RA (1970). A study of the composition of hen’s eggshell membranes. Ann Biol Anim Biochim Biophys 10: 13-25.
Draize JH, Woodard G, and Calvery H.D (1944). Methods for the study of irritation and toxicity of substances applied topically to the skin and mucous membranes, J Pharm Exp Ther 82: 377-390.
El-Maghraby GM, Ahmed A.A, and Osman M.A (2015). Penetration enhancers in proniosomes as a new strategy for enhanced transdermal drug delivery. Saudi Pharm J 23: 67-74.
Gyati Shilakari A, Parveen Kumar S, and Abhay A (2016). In Vitro and In Vivo Evaluation of Niosomal Formulation for Controlled Delivery of Clarithromycin, Scientifica (Cairo) 3: 1-10.
Ibrahim MMA, Sammour O.A, Hammad M.A and Megrab N.A (2009). In vitro evaluation of proniosomes as a drug carrier for flurbiprofen, AAPS Pharm Sci Tech 9: 782-790.
Jaafari MR, Bavarsad N, and Bazzaz BSF(2009). Effect of topical liposomes containing Paromomycin Sulfate in the course of Leishmania major infection in susceptible BALB/Mice anti-microbial agents and chemotherapy. Am Soc Microbiol 53: 2259-65.
Kaushik D, Mishra P.R and Talegaonkar S (2004). Provesicles as surrogate carrier for improved drug delivery, in: N.K. Jain (Ed.), Progress in Controlled and Novel Drug Delivery System, CBS Publishers and Distributors, India, pp-259-274.
Morrow DIJ, McCarron P.A, Woolfson A.D, and Donnelly R.F (2007). Innovative strategies for enhancing topical and transdermal drug delivery, Open Drug Deliv. J 1: 36-59.
Mah C, Zolotukhin T, Fraites T.Z, Dobson J, Batich C, and Byrne B.J (2002). Improved method of recombinant AAV2 delivery for systemic targeted gene therapy. Mol. Ther 6: 106-112.
Pankaj S, Rini T, and Dandagi P.M (2013). Formulation and evaluation of proniosome based drug delivery system of antifungal drug clotrimazole, IJPSN 8(1): 1945-51.
Rahman SA, Abdelmalak N.S, Badawi A, Elbayoumy T, Sabry N, and Ramly A.E (2015). Formulation of tretinoin-loaded topical proniosomes for treatment of acne: in-vitro characterization, skin irritation test and comparative clinical study. Drug Deliv. 22: 731-739.
Raj K (2012). Formulation and Evaluation of Proniosomal Gel in Ocular Drug. Current Research in Pharmaceutical Sciences 1: 42-47.
Ruan G, and Feng SS (2003). Preparation and Characterization of Poly (lactic acid) - poly (ethylene Glycol)-poly lactic acid (PLA-PEG-PLA) microspheres for the controlled release of Paclitaxel. Biomaterials 24: 5307-44).
Rahman SA, Abdelmalak NS, Badawi A, Elbayoumy T, Sabry N and El Ramly A (2015). Formulation of tretinoin-loaded topical proniosomes for treatment of acne: in-vitro characterization, skin irritation test and comparative clinical study. Drug Deliv 22(6): 731-9.
Sweetman SC (2005). Martindale- The Complete Drug Reference 34: 949.
Shamsher Ahmad S, Sabareesh M, Sai Krishna P, and Sudheer B (2011). Formulation and Evaluation of Lisinopril dehydrate transdermal proniosomal gels. Journal of Applied Pharma-ceutical Science 1(8): 181-185.
Swaminathan S, Pastero L, Serpe L, Trotta F, Vavia P, Aquilano D, Trotta G, Zara G., and Cavalli R (2010). Cyclodextrin-based nanosponges encapsulating camptothecin: physicochemical characterization, stability and cytotoxicity. Eur J Pharm Biopharm 74: 193.
Swaminathan S, Vavia P.R, Trotta F, Cavalli R, Tumbiolo S, Bertinetti L and Coluccia A (2013). Structural evidence of differential forms of nanosponges of betacyclodextrin and its effect on solubilization of a model drug. J Incl Phenom Macrocycl Chem 76: 201.
Singh S, Trivedi S, and Jain S (2010). Design and development of proniosome based transdermal delivery of ondansetron hydrochloride. Int J Pharm Biol Res 3(5): 191-201.
Thakur R, Anwer M.K, Shams M.S, Ali A, Khar R.K, Shakeel F and Taha E.I (2009). Proniosomal transdermal therapeutic system of losartan potassium: development and pharmacokinetic evaluation. J Drug Target 17: 442-449.
Vyas SP and Khar R.K (2004). Targeted and Controlled Drug Delivery-Novel Carrier Systems, first ed., CBS Publishers and Distributors, India: 249-279.
Vora B, Khopade A.J and Jain N.K (1998). Proniosomes based transdermal delivery of levonorgestrel for effective contraception. J Control Rel 54:149-165.
Wen MM, Farid RM and Kaseem AA (2014). Nano-proniosomes enhancing the transdermal delivery of mefenamic acid, J. Liposome Res 24: 280-289.
Yousuf M, Ahmad M, and Usman I Ali (2013). Ketotifen Fumarate and Salbutamol Sulphate Combined Transdermal Patch Formulations: In vitro release and Ex vivo Permeation Studies. Indian J Pharm Sci 75(5): 569-577.
Yasam VR, Jakki SL, Natarajan J, and Kuppusamy G (2014). A review on novel vesicular drug delivery: proniosomes, Drug Deliv 21: 243-249.
