Juan J Carrascal, GermÁn Matiz, Yolima Baena


BACKGROUND: Design of pharmaceutical forms of modified release is a current field of research, in which pharmaceutical companies invest enormous resources in searching for new raw materials of good performance, economic and wich can be processed in conventional equipments.

OBJECTIVES: Chemically modify by acetylation, Arracacia xanthorrhiza starch, and to physicochemically and pharmacotechnically characterize it, thereby evaluating its potential as a pharmaceutical excipient, in comparison with native starch.

METHODS: The chemical modification was performed through acetylation with acetic anhydride on different levels, determining following starch’s characteristics: degree of substitution, size and form of particles, its degree of crystallinity through X-ray diffraction, gelatinization temperature through Differential Scanning Calorimetry, swelling power and sorption isotherms by means of Enslin method, and its application as excipient in tablet production, using diclofenac as model drug.

RESULTS: On the third level of substitution, the morphology of modified-starch particles presented changes on their surface and all modified starches increased their particle average sizes, in comparison to native starch. Starch crystallinity was not altered by acetylation, and the DS increased as more acetic anhydride was added to the reaction. This modification caused a decrease of gelatinization temperature by approx. 9.45°C for A. xanthorrhiza starch modified to level III, in comparison to native starch. Swelling power and water uptake capacity increased with starch modification, being greater to higher DS. Dissolution studies conducted on tablets showed that diclofenac delivery occurs practically immediately when using native starch, while those made of acetylated starch complied with a zero-order kinetic, decreasing delivery-constant’s value by increasing starch acetylation levels.

CONCLUSIONS: The results suggest A. xanthorrhiza acetylated starches, as promising materials for the development of controlled-delivery matrix systems.


Acetylation; Starch; Arracacia xanthorrhiza; controlled delivery


Lordi NG. Sustained release dosage forms. In: Lachman L Lieberman HA & Kanig JL, editors. The Theory and Practice of Industrial Pharmacy. USA: Lea & Febiger;1986. p. 430-456.

Marinich JA, Ferrero C, Jiménez MR. Graft copolymers of ethyl methacrylate on waxy maize starch derivatives as novel excipients for matrix tablets: Drug release and fronts movement kinetics. European J Pharm Biopharm 2012; 80: 674–81.

Casas M, Ferrero C, Jiménez MR. Graft tapioca starch copolymers as novel excipients for controlled-release matrix tablets. Carbohydrate Polymers 2010; 80: 71–7.

Cubero N, Monferrer A, Villalta J. Aditivos alimentarios. 1th ed. Madrid (Esp): Mundi Prensa Libros S.A; 2002.

Siyawamwaya M, Choonara YE, Bijukumar D, Kumar P, Du Toit LC, Pillay V. A Review: Overview of Novel Polyelectrolyte Complexes as Prospective Drug Bioavailability Enhancers. Int. J of Polymeric Materials and Polymeric Biomaterials 2015; 64: 955–68.

Chen L, Li X, Li L, Guo S. Acetylated starch-based biodegradable materials with potential biomedical applications as drug delivery systems. Current Applied Physc 2007; 7: e90–e93.

Onofre FO, Wang YJ. Hydroxypropylated starches of varying amylose contents as sustained release matrices in tablets. Int J Pharmaceutics 2010; 385: 104–12.

Odeku OA, Picker-Freyer KM. Freeze-dried pregelatinized Dioscorea starches as tablet matrix for sustained reléase. J of Excipients and Food Chemicals. 2010; 1:21–32.

Lemieux M, Gosselin P, Mateescu MA. Carboxymethyl high amylose starch as excipient for controlled drug release: Mechanistic study and the influence of degree of substitution. Int J of Pharmaceutics. 2009; 382: 172–82.

Bello LA, Agama E, Zamudio PB, Méndez G, Rodriguez SL. Effect of low and high acetylation degree in the morphological, physicochemical and structural characteristics of barley starch. LWT - Food Science Technology 2010; 43: 1434 – 40.

Han F, Liu M, Gong H, Lü S, Ni B, Zhang B. Synthesis, characterization and functional properties of low substituted acetylated corn starch. Int J Biological Macromolecules 2012; 50: 1026–34.

Mirmoghtadaie L, Kadivar M, Shahedi M. Effects of cross-linking and acetylation on oat starch properties. Food Chemistry 2009; 116: 709–13.

Sodhi NS, Singh N. Characteristics of acetylated starches prepared using starches separated from different rice cultivars. J of Food Engineering 2005; 70: 117–27.

Rodriguez D, Baena Y, Espitia M, Caicedo Y, Córdoba Y, Mora C. Characterization of some physicochemical and pharmaceutical properties of starch obtained from yellow Peruvian parrot Arracacia xanthorriza. Revista Colombiana de Ciencias Quimico Farmaceuticas 2005; 34: 140–46.

Prieto J, Trejo CL, Prieto F, Méndez MA, Bello LA, Román AD. Acetilación y caracterización del almidón de cebada. Revista Latinoamericana de Recursos Naturales 2010; 6: 32–43.

Ayala G, Freitas IC, Vinicius RL, Quinta-Barbos AM, Sobral PJ. Physicochemical, morphological, and functional properties of flour and starch from peach palm (Bactris gasipaes K.) fruit. Starch - Stärke 2015; 67: 163-73.

González Z, Pérez E. Effect of Acetylation on Some Properties of Rice Starch. Starch - Stärke 2002; 54: 148–54.

Zuluaga MF, Baena Y, Mora CE, D’León LF. Physicochemical Characterization and Application of Yam Dioscorea cayenensis-rotundata Starch as a Pharmaceutical Excipient. Starch - Stärke 2007; 59: 307–17.

Jacobs PJ, Hemdane S, Dornez E, Delcour JA, Courtin CM. Study of hydration properties of wheat bran as a function of particle size. Food Chemistry 2015; 179: 296–304.

The United States Pharmacopoeia/ National Formulary, USP 39 / NF 34, Vol. I. The United States Pharmacopoeia Convention, Timbrook Parway, Rockville:2016. p.285,1334.

Xie F, Ji S, Cheng Z. In vitro dissolution similarity factor f2 and in vivo bioequivalence criteria , how and when do they match ? Using a BCS class II drug as a simulation example. European J of Pharmaceuticals Sciencies 2015; 66: 163–72.

Carrascal JJ. Acetilación del almidón de Arracacia xanthorrhiza y evaluación de su aplicación como posible auxiliar farmacéutico [Master's Thesis]. [Bogotá, Colombia]: Nacional de Colombia: 2013.

Bartz J, Goebel JT, Giovanaz MA, Zavareze ER, Artigas M, Guerra AR. Acetylation of barnyardgrass starch with acetic anhydride under iodine catalysis. Food Chemistry 2015; 178: 236–42.

Singh N, Chawla D, Singh J. Influence of acetic anhydride on physicochemical, morphological and thermal properties of corn and potato starch. Food Chemistry 2004; 86: 601–8.

Shah A, Masoodi FA, Gani A, Ashwar BA. Physicochemical, rheological and structural characterization of acetylated oat starches. LWT - Food Science Technology 2017; 80: 19–26.

Jeng L, An Y. Relationships between thermal, rheological characteristics and swelling power for various starches. J of Food Engineering 2001; 50: 141-48.

Singh J, Kaur L, Mccarthy OJ. Factors influencing the physico-chemical, morphological, thermal and rheological properties of some chemically modified starches for food applications — A review. Food Hydrocolloids 2007; 21: 1–22.

V.H. Barrera. Raíces y tubérculos andinos: alternativas para la conservación y uso sostenible en el Ecuador. Ecuador (Quito): Centro Internacional de la Papa CIP, editor; 2004.

Wang WC, Sastry SK. Starch gelatinization in ohmic heating. J of Food Engineering 1997; 34: 225–42.

Wootton M, Bamunuarachchi A. Application of Differential Scanning Calorimetry to Starch Gelatinization. I. Commercial Native and Modified Starches. Starch - Stärke. 1979; 31: 201–4.

Torruco J, Betancur D. Physicochemical and functional properties of makal Xanthosoma yucatanensis starch. Food Chemistry 2007; 101: 1319–26.

Diniz AC, Bagliotti A, Ferreira BS, Evangelista RC. Evaluation of retrograded starch as excipient for controlled release matrix tablets, J Drug Delivery Science and Technology 2017; 40: 83–94.

Peppas NA, Narasimhan B. Mathematical models in drug delivery: How modeling has shaped the way we design new drug delivery systems. J Control Release 2014; 190: 75–81.

Paixão P, Gouveia LF, Silva N, Morais JA. Evaluation of dissolution profile similarity – Comparison between the f2, the multivariate statistical distance and the f2 bootstrapping methods. European J of Pharmaceutics and Biopharmaceutics 2017; 112: 67–74.

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