Formulation and evaluation of orally disintegrating film (ODF) containing piperine-succinic acid cocrystal

Authors

  • Uswatul Hasanah Department of Pharmaceutics, Faculty of Pharmacy, Universitas Andalas
  • Lili Fitriani Department of Pharmaceutics, Faculty of Pharmacy, Universitas Andalas
  • Verlia Nisrina Putri Department of Pharmaceutics, Faculty of Pharmacy, Universitas Andalas
  • Erizal Zaini Department of Pharmaceutics, Faculty of Pharmacy, Universitas Andalas

DOI:

https://doi.org/10.12928/pharmaciana.v13i1.25286

Keywords:

Cocrystal piperine-succinic acid, orally disintegrating film, solvent casting, disintegration time

Abstract

Piperine is a type of alkaloid found in plants of the Piperaceae family, including Piper nigrum and Piper longum, which has numerous pharmacological properties and is being developed as a nutraceutical. However, its poor solubility makes delivering in effective doses for therapeutic purposes challenging. To overcome this limitation, the cocrystals of piperine and succinic acid was prepared, which are more soluble, and then formulated into orally disintegrating films (ODFs) for better delivery. The cocrystals were formed using the slurry method, while the ODFs were made using the solvent-casting method with different concentrations of hydroxypropyl methylcellulose (HPMC) and polyethylene glycol (PEG) 400. The resulting films were evaluated for various parameters, such as their organoleptic characteristics, weight and thickness uniformity, pH, moisture content, swelling properties, and disintegration time. The results showed that the ODF with 6% HPMC as a film-forming polymer and 0.6% PEG 400 as a plasticizer loaded with 10 mg of piperine in the form of piperine-succinic acid cocrystal was the best formula. This ODF formulation disintegrated in less than one minute and was found to be a good film with uniform content.

References

Vasavirama K, Upender M. Piperine: A Valuable Alkaloid From Piper Species. International Journal of Pharmacy and Pharmaceutical Science. 2014 Apr 5;6(4):34–8.

Tiwari A, Mahadik KR, Gabhe SY. Piperine: A comprehensive review of methods of isolation, purification, and biological properties. Med Drug Discov. 2020 Sep;7:100027.

Chopra B, Dhingra AK, Kapoor RP, Prasad DN. Piperine and Its Various Physicochemical and Biological Aspects: A Review. Open Chemistry Journal. 2016 Dec 30;3(1):75–96.

Gorgani L, Mohammadi M, Najafpour GD, Nikzad M. Piperine-The Bioactive Compound of Black Pepper: From Isolation to Medicinal Formulations. Compr Rev Food Sci Food Saf. 2017 Jan;16(1):124–40.

Vijayakumar RS, Surya D, Nalini N. Antioxidant efficacy of black pepper ( Piper nigrum L.) and piperine in rats with high fat diet induced oxidative stress. Redox Report. 2004 Apr 19;9(2):105–10.

Zarai Z, Boujelbene E, ben Salem N, Gargouri Y, Sayari A. Antioxidant and antimicrobial activities of various solvent extracts, piperine and piperic acid from Piper nigrum. LWT - Food Science and Technology. 2013 Mar;50(2):634–41.

Umadevi P, Deepti K, Venugopal DVR. Synthesis, anticancer and antibacterial activities of piperine analogs. Medicinal Chemistry Research. 2013 Nov 28;22(11):5466–71.

Katiyar SS, Muntimadugu E, Rafeeqi TA, Domb AJ, Khan W. Co-delivery of rapamycin- and piperine-loaded polymeric nanoparticles for breast cancer treatment. Drug Deliv. 2016 Sep 1;23(7):2608–16.

Smilkov K, Ackova DG, Cvetkovski A, Ruskovska T, Vidovic B, Atalay M. Piperine: Old Spice and New Nutraceutical? Curr Pharm Des. 2019 Aug 19;25(15):1729–39.

Dudeja P, Gupta RK. Nutraceuticals. In: Food Safety in the 21st Century. Elsevier; 2017. p. 491–6.

Télessy IG. Nutraceuticals. In: The Role of Functional Food Security in Global Health. Elsevier; 2019. p. 409–21.

Oladimeji FA, Adegbola AJ, Onyeji CO. Appraisal of Bioenhancers in Improving Oral Bioavailability: Applications to Herbal Medicinal Products. J Pharm Res Int. 2018 Nov 29;24(4):1–23.

Alatas F, Ratih H, Kurnia H, Soewandhi SN. Solubility Enhancement of Clozapine Through Co-Crystal Formation with Isonicotinamide. Indonesian Journal of Pharmaceutics. 2019 Nov 26;2(1).

Aungst BJ, Nguyen NH, Taylor NJ, Bindra DS. Formulation and Food Effects on the Oral Absorption of a Poorly Water Soluble, Highly Permeable Antiretroviral Agent. J Pharm Sci. 2002 Jun;91(6):1390–5.

Ezawa T, Inoue Y, Murata I, Takao K, Sugita Y, Kanamoto I. Characterization of the Dissolution Behavior of Piperine/Cyclodextrins Inclusion Complexes. AAPS PharmSciTech. 2018 Feb 25;19(2):923–33.

Zafar F, Jahan N, Bhatti H. Increased Oral Bioavailability of Piperine from an Optimized Piper nigrum Nanosuspension. Planta Med. 2019 Feb 24;85(03):249–57.

Zaini E, Afriyani, Fitriani L, Ismed F, Horikawa A, Uekusa H. Improved Solubility and Dissolution Rates in Novel Multicomponent Crystals of Piperine with Succinic Acid. Sci Pharm. 2020 Apr 13;88(2):21.

Sari YN, Zaini E, Ismed F. Peningkatan Laju Disolusi Piperine dengan Pembentukan Multikomponen Kristal Menggunakan Asam Nikotinat. Jurnal Sains Farmasi & Klinis. 2019 Aug 28;6(2):180.

Zaini E, Riska D, Oktavia MD, Ismed F, Fitriani L. Improving Dissolution Rate of Piperine by Multicomponent Crystal Formation with Saccharin. Res J Pharm Technol. 2020;13(4):1928.

Siddiqui MDN, Garg G, Sharma PK. A Short Review on “A Novel Approach in Oral Fast Dissolving Drug Delivery System and Their Patents.” Advan Biol Res. 2011;5(6):291–303.

Downloads

Published

2023-04-03

Issue

Vol. 13 No. 1 (2023): Pharmaciana

Section

Pharmaceutics and Pharmaceutical Technology

License

Authors who publish with Pharmaciana agree to the following terms:

  1. Authors retain copyright and grant the journal the right of first publication with the work simultaneously licensed under a Creative Commons Attribution License (CC BY-SA 4.0) that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal. 
  2. Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
  3. Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work.