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Pre-exposure prophylactic mucoadhesive sodium alginate microsphere laden pessaries for intravaginal delivery of tenofovir disoproxil fumarate.
Avlani, Dhruti; Shivakumar, H N; Kumar, Avichal; Prajila, A; Baraka, Babiker Bashir Haroun; Bhagya, V.
Afiliación
  • Avlani D; Department of Pharmaceutics, Dr. Prabhakar B Kore Basic Science Research Center, Off-campus, KLE College of Pharmacy (A constituent unit of KAHER-Belagavi), Rajajinagar, Bengaluru 560010, Karnataka, India.
  • Shivakumar HN; Department of Pharmaceutics, Dr. Prabhakar B Kore Basic Science Research Center, Off-campus, KLE College of Pharmacy (A constituent unit of KAHER-Belagavi), Rajajinagar, Bengaluru 560010, Karnataka, India. Electronic address: shivakumarhn@gmail.com.
  • Kumar A; Department of Pharmaceutics, Dr. Prabhakar B Kore Basic Science Research Center, Off-campus, KLE College of Pharmacy (A constituent unit of KAHER-Belagavi), Rajajinagar, Bengaluru 560010, Karnataka, India.
  • Prajila A; Department of Pharmaceutics, Dr. Prabhakar B Kore Basic Science Research Center, Off-campus, KLE College of Pharmacy (A constituent unit of KAHER-Belagavi), Rajajinagar, Bengaluru 560010, Karnataka, India.
  • Baraka BBH; Department of Pharmacology, Dr. Prabhakar B Kore Basic Science Research Center, Off-campus, KLE College of Pharmacy (A constituent unit of KAHER-Belagavi), Rajajinagar, Bengaluru 560010, Karnataka, India.
  • Bhagya V; Department of Pharmacology, Dr. Prabhakar B Kore Basic Science Research Center, Off-campus, KLE College of Pharmacy (A constituent unit of KAHER-Belagavi), Rajajinagar, Bengaluru 560010, Karnataka, India.
Int J Biol Macromol ; 258(Pt 1): 128816, 2024 Feb.
Article en En | MEDLINE | ID: mdl-38114000
ABSTRACT
The research aimed to develop novel bioadhesive sodium alginate (Na-Alg) microspheres laden pessaries for intravaginal delivery of tenofovir disoproxil fumarate (TDF), to overcome limitations of conventional dosage forms. Twelve batches of microspheres formulated by emulsification gelation method indicated that drug-polymer ratios and polymer type affected particle size, drug release, and entrapment efficiency (%EE). Microspheres of batch EH-8 with drug polymer ratio of 14 containing equal amounts of Na-Alg and HPMC K100M displayed optimal %EE (62.09 ± 1.34 %) and controlled drug release (97.02 ± 4.54 % in 12 h). Particle size analysis in Matersizer indicated that microspheres (EH-8) displayed a surface-mean diameter of 11.06 ± 0.18 µm. Ex-vivo mucoadhesion studies on rabbit mucosa indicated that microspheres (EH-8) adhered well for 12 h. Microspheres integrated into pessaries displayed a sustained release profile (95.31 ± 1.37 % in 12 h) in simulated vaginal fluid. In vivo studies in rabbits indicated that pessaries displayed a significantly higher Cmax (41.18 ± 3.57 ng/mL) (P < 0.005) and reduced Tmax (1.00 ± 0.01 h) (P < 0.0001) of TDF concentrations in vaginal fluid compared to oral tablets. The microparticulate pessaries with the ability to elicit higher vaginal fluid levels in the crucial initial hours of insertion demonstrates a potential novel platform to offer better self-protection to HIV-negative women against HIV during sexual intercourse.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Infecciones por VIH / Alginatos Límite: Animals / Female / Humans Idioma: En Revista: Int J Biol Macromol Año: 2024 Tipo del documento: Article País de afiliación: India Pais de publicación: Países Bajos
Texto completo
Añadir a Mi BVS
Imprimir
XML
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Infecciones por VIH / Alginatos Límite: Animals / Female / Humans Idioma: En Revista: Int J Biol Macromol Año: 2024 Tipo del documento: Article País de afiliación: India Pais de publicación: Países Bajos