PMID- 20190525 OWN - NLM STAT- MEDLINE DCOM- 20100429 LR - 20190724 IS - 0031-6903 (Print) IS - 0031-6903 (Linking) VI - 130 IP - 3 DP - 2010 Mar TI - Crystalline drug aconitine-loaded poly(d,l-lactide-coglycolide) nanoparticles: preparation and in vitro release. PG - 409-18 AB - This paper reports both the optimization of aconitine entrapment and its release from biodegradable poly(d,l-lactide-coglycolide) (PLGA) nanoparticles prepared using the O/W single-emulsion/solvent-evaporation technique. The influence of several parameters, such as the initial aconitine mass, aqueous-phase pH, volume ratio of aqueous/organic phase (W/O), PLGA concentration in the organic phase, etc., on aconitine encapsulation were investigated. The optimized nanoparticles had an entrapment efficiency of 88.40+/-3.02% with drug loading capacity of 9.42+/-2.93%. Crystallization growth, which played a crucial role in hindering the incorporation of aconitine into the polymer carrier, was proposed. Differential scanning calorimetry and X-ray powder diffraction demonstrated that aconitine existed in an amorphous state or as a solid solution in the polymeric matrix. The in vitro release profiles exhibited a sustained release of aconitine from nanoparticles and a pH-dependent character in phosphate-buffered saline with different pH values. Moreover, aconitine-loaded PLGA nanoparticles could lead to improvement in the stability of aconitine. This work demonstrated the feasibility of encapsulating aconitine into PLGA nanoparticles using the O/W single-emulsion/solvent-evaporation technique. FAU - Xu, Xuefan AU - Xu X AD - Key Laboratory of Drug Targeting of the Ministry of Education, West China School of Pharmacy, Sichuan University, China. FAU - Xiang, Qingyu AU - Xiang Q FAU - He, Zhiyao AU - He Z FAU - Liu, Yuehua AU - Liu Y FAU - Zhou, Dan AU - Zhou D FAU - Qin, Xuan AU - Qin X FAU - Fan, Tingting AU - Fan T FAU - Zhang, Zhirong AU - Zhang Z FAU - Huang, Yuan AU - Huang Y LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - Japan TA - Yakugaku Zasshi JT - Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan JID - 0413613 RN - 0 (Delayed-Action Preparations) RN - 0 (Nanocapsules) RN - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer) RN - 26009-03-0 (Polyglycolic Acid) RN - 33X04XA5AT (Lactic Acid) RN - X8YN71D5WC (Aconitine) SB - IM MH - *Aconitine/administration & dosage/pharmacokinetics MH - Chemistry, Pharmaceutical MH - Crystallization MH - Delayed-Action Preparations MH - *Drug Delivery Systems MH - Drug Stability MH - Hydrogen-Ion Concentration MH - In Vitro Techniques MH - *Lactic Acid MH - *Nanocapsules MH - *Nanoparticles MH - Nanotechnology/methods MH - *Polyglycolic Acid MH - Polylactic Acid-Polyglycolic Acid Copolymer EDAT- 2010/03/02 06:00 MHDA- 2010/04/30 06:00 CRDT- 2010/03/02 06:00 PHST- 2010/03/02 06:00 [entrez] PHST- 2010/03/02 06:00 [pubmed] PHST- 2010/04/30 06:00 [medline] AID - JST.JSTAGE/yakushi/130.409 [pii] AID - 10.1248/yakushi.130.409 [doi] PST - ppublish SO - Yakugaku Zasshi. 2010 Mar;130(3):409-18. doi: 10.1248/yakushi.130.409.