Document Type : CASE STUDY


Department of Chemistry, Faculty of Mathematics and Natural Sciences, Universitas Indonesia, Depok, West Java, Indonesia


Nifedipine is a hypertension drug must be consumed three times a day due to its low oral bioavailability. One way of developing a controlled drug delivery system is making nifedipine microcapsules by using environmentally friendly polymers of polylactic acid and polycaprolactone via the evaporation method using oil-in-water solvents. Polylactic acid and polycaprolactone can be said to be environmentally friendly polymers, because they can be degraded naturally in nature both in the biotic, and abiotic environment, or microorganism. In this study, polylactic acid, Polycaprolactone, and nifedipine were dissolved in dichloromethane solvent; then, an emulsifier was added for the emulsification stage. After passing through the dispersion stage for the process of compaction of the microcapsules by solvent evaporation, the microcapsules were filtered. Microcapsules were characterized using particle size analysis, X-ray diffractometry, and scanning electron microscopy, respectively. The drug release percentage was determined by dissolving microcapsules for 55 hours using a buffer at the potential of hydrogen 1.2 and pH 7.4 as dissolution media. In this study, all variations in the composition of polyblend resulted in a percent efficiency of encapsulation ranging from 78.82%-89.84%, and percent release ranging from 6.80%-39.07%. The composition of 100% polylactic acid produces the highest percent encapsulation efficiency of 89.84% but produces the lowest percentage of drug release at 6.80%. The best composition obtained was polylactic acid: polycaprolactone 1:9 (weight per weight), with a percent release of 39.07% and percent encapsulation of 78.82%. Microcapsule solids produced are approximately 96%. Particle Size of microcapsule ranges at 0.5 μM.

Graphical Abstract

Environmental friendly carrier material for nifedipine as hypertension drug


  • Poly-DL-lactic acid and polycaprolactone are suitable to be used as a matrix for nifedipine carrier due to their lipophilicity;
  • The higher the composition of polycaprolactone in the matrix, the drug release percentage will be higher due to the polycaprolactone high permeabilities properties;
  • The higher polycaprolactone composition in the matrix will create many holes in the matrix;
  • The greater poly-DL-lactic acid composition in the matrix, the burst release effect will be smaller.


Main Subjects

Agarwal, M.; Koelling, K.W.; Chalmers, J.J., (1998). Characterization of the degradation of polylactic acid polymer in a solid substrate environment. Biotechnol. Progr., 14(3): 517-526 (10 pages).

Ahmed, J.; Varshney, S.K., (2011). Polylactides-chemistry, properties, and green packaging technology: A review. Int. J. Food Prop., 14(1): 37-58 (22 pages).

Anne, B., (2011). Environmental-Friendly Biodegradable Polymers and Composites. Integr. Waste Manage., 1: 341-365 (25 pages).

Bhowmik, D.; Gopinath, H.; Kumar, B.P.; Duraivel, S.; Kumar, K.P.S., (2012). Controlled Release Drug Delivery Systems. The Pharma Innovation, 1(10): 24-32 (9 pages).

Bikiaris, D., (2011). Evaluating the effects of crystallinity in new biocompatible polyester nanocarriers on drug release behavior. Int. J. Nanomed., 6: 3021-3032 (12 pages).

Cayot, N.; Lafarge, C.; Bou-Maroun, E.; Cayot, P., (2016). Substitution of carcinogenic solvent dichloromethane for the extraction of volatile compounds in a fat-free model food system. J. Chromatogr., 1456: 77-88 (12 pages).

Chen, C.; Chueh, J.; Tseng, H.; Huang, H.; Lee, S., (2003). Preparation and characterization of biodegradable PLA polymeric blends. Biomater., 24(7): 1167-1173 (7 pages).

Cole, F.W., (1983). Reservoir Engineering Manual, Gulf Publishing Company, Texas.

Davarani, S.S.H.; Rezayati-zad, Z.; Taheri, A.; Rahmatian, N., (2017). Highly selective solid phase extraction and preconcentration of Azathioprine with nano-sized imprinted polymer based on multivariate optimization and its trace determination in biological and pharmaceutical samples, Mater Sci. Eng. C., 71: 572-583 (12 pages).

Deshmukh, K.; Ahamed, M.B.; Deshmukh, R.R.; Pasha, S.K.K.; Bhagat, P.R.; Chidambaram, K., (2017). 3 - biopolymer composites with high dielectric performance: interface engineering. Biopolym. Compos. Electron., 27-127 (101 pages).

Dorgan, J.R.; Lehermeier, H.J.;  Palade, L.-I.; Cicero, J., (2001). Polylactides: properties and prospects of an environmentally benign plastic from renewable resources. Macromol. Symp., 175(1): 55-66 (12 pages).

Elliott, W.J.; Ram, C.V.S., (2011). Calcium channel blockers. J. Clin. Hypertens., 13: 687-689 (3 pages). 

Ge, H.; Hu, Y.; Yang, S.; Jiang, X.; Yang, C., (2000). Preparation, characterization, and drug release behaviors of drug-loaded Ɛ-caprolactone/L-lactide copolymer nanoparticles. J. Appl. Polym. Sci., 75: 874-882 (9 pages).

Godfraind, T., (1994). Calcium antagonists and vasodilation. Pharmac. Ther., 64(1): 37-75 (39 pages).

Jackson, M.; Wagnieres, G.; Mantsch, H.H., (2017). IR, Medical Science Applications. Encycl. Spectrosc. Spectrom., 3: 479-487 (9 pages).

Javed, I.; Ranjha, N.M.; Mahmood, K.; Kashif, S.; Rehman, M.; Usman, F., (2014). Drug release optimization from microparticles of poly(ε-caprolactone) and hydroxypropyl methylcellulose polymeric blends: Formulation and characterization. J. Drug Delivery Sci. Technol., 24(6): 607-612 (6 pages).

Jayanthi, B.; Manna, P.K.; Madhusudhan, S.; Mohanta, G.P.; Manavalan, R., (2011). Per oral extended release products: An overview. J. Appl. Pharm. Sci., 1(2): 50-55 (6 pages).

Kemala, T.; Budianto, E.; Soegiyono, B., (2012). Preparation and characterization of microspheres based on blend of poly(lactic acid) and poly(ε-caprolactone) with poly(vinyl alcohol) as emulsifier. Arabian J. Chem., 5(1): 103-108 (6 pages).

Kirarli, T., (1995). Review article comparison of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory animals. Biopharm. Drug Dispos., 16: 351–380 (30 pages).

Leja, K.; Lewandowicz, G., (2010). Polymer Biodegradation and Biodegradable Polymers – a Review. Pol. J. Environ. Stud., 19: 255–266 (12 pages).

Li, M.; Rouaud, O.; Poncelet, D., (2008). Microencapsulation by solvent evaporation: State of the art for process engineering approaches. Int. J. Pharm., 363(1-2): 26-39 (14 pages).

Liechty, W.B.; Kryscio, D.R.; Slaughter, B.V.; Peppas, N.A., (2010). Polymers for drug delivery systems. Annu. Rev. Chem. Biomol. Eng., 1: 149−173 (25 pages).

Lu, Y.; Chen, S.C., (2004). Micro and nano-fabrication of biodegradable polymers for drug delivery, Adv. Drug Delivery Rev., 56(11): 1621-1633 (13 pages).

Lunt, J., (1998). Large-scale production, properties and commercial applications of poly lactic acid polymers. Polym. Degrad. Stab., 59(1-3): 145-152 (8 pages).

Mehta, A.C., (1993). Dissolution testing of tablet and capsule dosage forms. J. Clin. Pharm. Ther. 18(6): 415–420 (6 pages).

Motiwalla, M.J.; Punyarthi, P.P.; Mehta, M.K.; D’Souza, J.S.; Kelkar-Mane, V., (2013). Studies on degradation efficiency of polycaprolactone by a naturally-occurring bacterium. J. Environ. Biol., 34(1): 43-49 (7 pages).

Nair, L.S.; Laurencin, C.T., (2007). Biodegradable polymers as biomaterials, Prog. Polym. Sci., 32(8-9): 762-798 (37 pages).

Narang, A.S.; Delmarre, D.; Gao, D., (2007). Stable drug encapsulation in micelles and microemulsions. Int. J. Pharm., 345(1-2): 9-25 (17 pages).

Nishida, H.; Tokiwa, Y., (1993). Distribution of poly(β-hydroxybutyrate) and poly(ε-caprolactone)aerobic degrading microorganisms in different environments. J. Environ. Polym. Degrad., 1: 227–233 (7 pages).

Park, T.G., (1994). Degradation of Poly(D,L-Lactic acid) microsphere: effect of molecular weight. J. Control Release, 30(2): 161-173 (13 pages).

Prathusha, P.; Bhargavi, L.; J, B.D.; Choudhary, Y.; Reddy, K.; Patil, A.; Monsuur, F., (2015). Formulation development and in-vitro evaluation of Nifedipine sublingual tablets using mesoporous silica. Pharma Innovation J., 4(10): 76-82 (7 pages).

Ray, S.S., (2013). Introduction to environmentally friendly polymer nanocomposites. Environ. Friendly Polym. Nanocomposites, 3-24 (22 pages).

Rasal, R.M.; Janorkar, A.V.; Hirt, D.E., (2010). Poly(lactic acid) modifications. Prog. Polym. Sci.,35(3): 338–356 (19 pages).

Salomone, S.; Silva, C.L.M.; Morel, N.; Godfraind, T., (1996). Facilitation of the vasorelaxant action of calcium antagonists by basal nitric oxide in depolarized artery. Naunyn- Schmiedeberg's Arch. Pharmacol. 354(4): 505–512 (8 pages).

Sharma, N.; Madan, P.; Lin, S., (2016). Effect of process and formulation variables on the preparation of parenteral paclitaxel-loaded biodegradable polymeric nanoparticles: A co-surfactant study. Asian J. Pharm. Sci., 11(3): 404-416 (13 pages).

Shi, D.X.; Sun, J.P.; Gun, H.Z., (2018). Preparation of Porous Polylactide Microspheres and Their Application in Tissue Engineering. Chin. J. Polym. Sci., 36: 712-719 (8 pages).

Sin, L.T.; Tueen, B.S., (2019). Environmental Assessment of Poly(Lactic Acid) and International Standards. Polylactic Acid, 2: 365-387 (23 pages).

Sinha, V.R.; Bansal, K.; Kaushik, R.; Kumria, R.; Trehan, A., (2004). Poly- caprolactone microspheres and nanospheres: an overview. Int. J. Pharm., 278(1): 1–23 (23 pages).

Swarbrick, J.; Hill, C.; Carolina, N., (2006). Molecular Interaction in Surfactant Solutions: From Micelles to Microemulsions, University of Florida.

Tokiwa, Y.; Suzuki, T., (1977). Hydrolysis of polyesters by lipases.Nat., 270: 76-78 (3 pages).

Tiwari, S.; Verma, P., (2011). Microencapsulation technique by solvent evaporation method (Study of effect of process variables). Int. J. Pharm. Life Sci., 2(8): 998-1005 (8 pages).

Velde, K.V.; Kiekens, P., (2001). Biopolymer overview of several properties and consequences on their applications. Polym. Test., 21(4): 433-442 (10 pages).

Wati, E.P.G.; Hayatunnufus, R.; Budianto, E., (2018). Characterization and Efficiency Test of Nifedipine (NIF) Microencapsulation Using Polyblend of Poly(Lactic Acid) and Poly(Ɛ-Caprotactone). Mater. Sci. Forum, 947: 26-31 (6 pages).

Woodruff, M.A.; Hutmacher, D.W., (2010). Progress in polymer science The return of a forgotten polymer — Polycaprolactone in the 21st century. Progress Polym. Sci., 35(10): 1217–1256 (40 pages).

Yeo, Y.; Park, K., (2004). Control of Encapsulation Efficiency and Initial Burst in Polymeric Microparticle Systems. Arch. Pharmacal Res., 27: 1-12 (12 pages).

Young, R.C.; Schumann, R.; Zhang, P., (2001). Nifedipine block of capacitative calcium entry in cultured human uterine smooth-muscle cells. J. Soc. Gynecol. Invest., 210-215 (6 pages).

Young, R.J.; Lovell, P.A., (2011). Introduction to Polymers: Third Edition, CRC Press, Boca Raton.

Letters to Editor

GJESM Journal welcomes letters to the editor for the post-publication discussions and corrections which allows debate post publication on its site, through the Letters to Editor. Letters pertaining to manuscript published in GJESM should be sent to the editorial office of GJESM within three months of either online publication or before printed publication, except for critiques of original research. Following points are to be considering before sending the letters (comments) to the editor.

[1] Letters that include statements of statistics, facts, research, or theories should include appropriate references, although more than three are discouraged.
[2] Letters that are personal attacks on an author rather than thoughtful criticism of the author’s ideas will not be considered for publication.
[3] Letters can be no more than 300 words in length.
[4] Letter writers should include a statement at the beginning of the letter stating that it is being submitted either for publication or not.
[5] Anonymous letters will not be considered.
[6] Letter writers must include their city and state of residence or work.
[7] Letters will be edited for clarity and length.