Electrosprayed core-shell solid dispersions of acyclovir fabricated using an epoxy-coated concentric spray head.
A novel structural solid dispersion (SD) taking the form of core-shell microparticles for poorly water-soluble drugs is reported for the first time. Using polyvinylpyrrolidone (PVP) as a hydrophilic polymer matrix, the SDs were fabricated using coaxial electrospraying (characterized by an epoxy-coated concentric spray head), although the core fluids were unprocessable using one-fluid electrospraying. Through manipulating the flow rates of the core drug-loaded solutions, two types of core-shell microparticles with tunable drug contents were prepared. They had average diameters of 1.36±0.67 and 1.74±0.58 μm, and were essentially a combination of nanocomposites with the active ingredient acyclovir (ACY) distributed in the inner core, and the sweeter sucralose and transmembrane enhancer sodium dodecyl sulfate localized in the outer shell. Differential scanning calorimetry and X-ray diffraction results demonstrated that ACY, sodium dodecyl sulfate, and sucralose were well distributed in the PVP matrix in an amorphous state because of favorable second-order interactions. In vitro dissolution and permeation studies showed that the core-shell microparticle SDs rapidly freed ACY within 1 minute and promoted nearly eightfold increases in permeation rate across the sublingual mucosa compared with raw ACY powders.
School of Medical Instrument and Food Engineering, Shanghai, People's Republic of China.
Zhe-Peng
ZP
Liu
Tin Ka Ping College of Science, Shanghai, People's Republic of China.
Lei
L
Cui
School of Materials Science and Engineering, University of Shanghai for Science and Technology, Shanghai, People's Republic of China.
Deng-Guang
DG
Yu
School of Medical Instrument and Food Engineering, Shanghai, People's Republic of China.
Zhuan-Xia
ZX
Zhao
School of Medical Instrument and Food Engineering, Shanghai, People's Republic of China.
Lan
L
Chen
D000212:Acyclovir / Q000737:chemistry*; D000818:Animals; D000998:Antiviral Agents / Q000737:chemistry; D002214:Capsules / Q000138:chemical synthesis*; D004058:Diffusion; D004595:Electroplating / Q000295:instrumentation* / Q000379:methods; D004655:Emulsions / Q000138:chemical synthesis*; D004853:Epoxy Resins / Q000737:chemistry*; D004867:Equipment Design; D019544:Equipment Failure Analysis; D005740:Gases; D066298:In Vitro Techniques; D044085:Microfluidics; D009061:Mouth Mucosa / Q000737:chemistry*; D065568:Oral Mucosal Absorption; D010316:Particle Size; D011145:Polyvinyls / Q000737:chemistry*; D011759:Pyrrolidines / Q000737:chemistry*; D013552:Swine; D014018:Tissue Distribution
D000998:Antiviral Agents; D002214:Capsules; D004655:Emulsions; D004853:Epoxy Resins; D005740:Gases; D011145:Polyvinyls; D011759:Pyrrolidines; C505150:poly(N-vinylpyrrolidine); D000212:Acyclovir
coaxial electrospraying; core–shell microparticle; epoxy-coated spray head; poorly water-soluble drug; solid dispersion