Mucoadhesive Microspheres of Maraviroc and Tenofovir Designed for Pre-Exposure Prophylaxis of HIV-1: An in vitro Assessment of the Effect on Vaginal Lactic Acid Bacteria Microflora

Sabdat O Ekama,1,2 Margaret O Ilomuanya,1 Chukwuemeka P Azubuike,1 Tajudeen A Bamidele,2 Muinah A Fowora,2 Oluwagbemiga O Aina,2 Oliver C Ezechi,2 Cecilia I Igwilo1 1Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, University of Lagos, Lagos, Nigeria; 2Clinical Science...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Ekama SO, Ilomuanya MO, Azubuike CP, Bamidele TA, Fowora MA, Aina OO, Ezechi OC, Igwilo CI
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2021
Materias:	vaginal microbicides hiv prevention lactobacillus fermentum enterococcus faecalis. Immunologic diseases. Allergy RC581-607
Acceso en línea:	https://doaj.org/article/ff1d6fe759434abfaea9640684009ac0
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:ff1d6fe759434abfaea9640684009ac0
record_format	dspace
spelling	oai:doaj.org-article:ff1d6fe759434abfaea9640684009ac02021-12-02T14:25:42ZMucoadhesive Microspheres of Maraviroc and Tenofovir Designed for Pre-Exposure Prophylaxis of HIV-1: An in vitro Assessment of the Effect on Vaginal Lactic Acid Bacteria Microflora1179-1373https://doaj.org/article/ff1d6fe759434abfaea9640684009ac02021-04-01T00:00:00Zhttps://www.dovepress.com/mucoadhesive-microspheres-of-maraviroc-and-tenofovir-designed-for-pre--peer-reviewed-article-HIVhttps://doaj.org/toc/1179-1373Sabdat O Ekama,1,2 Margaret O Ilomuanya,1 Chukwuemeka P Azubuike,1 Tajudeen A Bamidele,2 Muinah A Fowora,2 Oluwagbemiga O Aina,2 Oliver C Ezechi,2 Cecilia I Igwilo1 1Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, University of Lagos, Lagos, Nigeria; 2Clinical Sciences Department, Nigerian Institute of Medical Research, Lagos, NigeriaCorrespondence: Sabdat O EkamaClinical Sciences Department, Nigerian Institute of Medical Research, 6 Edmund Crescent, P.M.B 2013, Yaba, Lagos, NigeriaTel +234 8134761356Email sabdatekama@nimr.gov.ngPurpose: To formulate and evaluate microspheres of the antiretroviral drugs maraviroc and tenofovir intended for a candidate vaginal microbicide and assess its effect on the vaginal lactic acid bacteria microflora.Methods: Ionic gelation technique was used to formulate maraviroc and tenofovir microspheres with subsequent characterization. The effect of varying concentrations of the polymer, crosslinking agent and the curing time on the outcome variables viz: particle size, mucoadhesion and encapsulation efficiency were investigated. Lactic acid bacteria were isolated from the vagina of healthy women using standard microbiologic methods. The analysis of their 16S rRNA sequence data identified Lactobacillus fermentum and Enterococcus faecalis strains which were assigned GenBank accession numbers. The efficacy of the microspheres on HIV-1BaL strain was evaluated using TZM-bl indicator cells.Results: The optimal maraviroc and tenofovir microspheres had particle sizes of (434.82 μm and 456.18 μm), mucoadhesion of (93.3% and 90%) and encapsulation efficiency (92.80% and 78.9%) respectively. Maraviroc release kinetics followed a zero-order model and tenofovir was released via Higuchi model. The assay of a 1 mg/mL suspension of the microspheres on the strains of Lactobacillus fermentum and Enterococcus faecalis showed a viability of 93.9% and 89.7%, respectively. There was a statistically significant difference between the mean absorbance readings of the test agent and that of the positive control (P = 0.001). The microspheres elicited a progressive decline in HIV infectivity until at a concentration of 1 μg/mL.Conclusion: The antiretroviral drugs loaded in the microspheres, had good mucoadhesion which is a potential for prolonged residence time in the vagina. The antiretroviral drugs were adequately released from the microspheres and showed efficacy against the HIV-1 BaL virus strain. There was no significant disruption in the growth of the lactic acid bacteria which constitute valuable bacteria microflora of the vagina.Keywords: vaginal microbicides, HIV prevention, Lactobacillus fermentum, Enterococcus faecalisEkama SOIlomuanya MOAzubuike CPBamidele TAFowora MAAina OOEzechi OCIgwilo CIDove Medical Pressarticlevaginal microbicideshiv preventionlactobacillus fermentumenterococcus faecalis.Immunologic diseases. AllergyRC581-607ENHIV/AIDS: Research and Palliative Care, Vol Volume 13, Pp 399-413 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	vaginal microbicides hiv prevention lactobacillus fermentum enterococcus faecalis. Immunologic diseases. Allergy RC581-607
spellingShingle	vaginal microbicides hiv prevention lactobacillus fermentum enterococcus faecalis. Immunologic diseases. Allergy RC581-607 Ekama SO Ilomuanya MO Azubuike CP Bamidele TA Fowora MA Aina OO Ezechi OC Igwilo CI Mucoadhesive Microspheres of Maraviroc and Tenofovir Designed for Pre-Exposure Prophylaxis of HIV-1: An in vitro Assessment of the Effect on Vaginal Lactic Acid Bacteria Microflora
description	Sabdat O Ekama,1,2 Margaret O Ilomuanya,1 Chukwuemeka P Azubuike,1 Tajudeen A Bamidele,2 Muinah A Fowora,2 Oluwagbemiga O Aina,2 Oliver C Ezechi,2 Cecilia I Igwilo1 1Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, University of Lagos, Lagos, Nigeria; 2Clinical Sciences Department, Nigerian Institute of Medical Research, Lagos, NigeriaCorrespondence: Sabdat O EkamaClinical Sciences Department, Nigerian Institute of Medical Research, 6 Edmund Crescent, P.M.B 2013, Yaba, Lagos, NigeriaTel +234 8134761356Email sabdatekama@nimr.gov.ngPurpose: To formulate and evaluate microspheres of the antiretroviral drugs maraviroc and tenofovir intended for a candidate vaginal microbicide and assess its effect on the vaginal lactic acid bacteria microflora.Methods: Ionic gelation technique was used to formulate maraviroc and tenofovir microspheres with subsequent characterization. The effect of varying concentrations of the polymer, crosslinking agent and the curing time on the outcome variables viz: particle size, mucoadhesion and encapsulation efficiency were investigated. Lactic acid bacteria were isolated from the vagina of healthy women using standard microbiologic methods. The analysis of their 16S rRNA sequence data identified Lactobacillus fermentum and Enterococcus faecalis strains which were assigned GenBank accession numbers. The efficacy of the microspheres on HIV-1BaL strain was evaluated using TZM-bl indicator cells.Results: The optimal maraviroc and tenofovir microspheres had particle sizes of (434.82 μm and 456.18 μm), mucoadhesion of (93.3% and 90%) and encapsulation efficiency (92.80% and 78.9%) respectively. Maraviroc release kinetics followed a zero-order model and tenofovir was released via Higuchi model. The assay of a 1 mg/mL suspension of the microspheres on the strains of Lactobacillus fermentum and Enterococcus faecalis showed a viability of 93.9% and 89.7%, respectively. There was a statistically significant difference between the mean absorbance readings of the test agent and that of the positive control (P = 0.001). The microspheres elicited a progressive decline in HIV infectivity until at a concentration of 1 μg/mL.Conclusion: The antiretroviral drugs loaded in the microspheres, had good mucoadhesion which is a potential for prolonged residence time in the vagina. The antiretroviral drugs were adequately released from the microspheres and showed efficacy against the HIV-1 BaL virus strain. There was no significant disruption in the growth of the lactic acid bacteria which constitute valuable bacteria microflora of the vagina.Keywords: vaginal microbicides, HIV prevention, Lactobacillus fermentum, Enterococcus faecalis
format	article
author	Ekama SO Ilomuanya MO Azubuike CP Bamidele TA Fowora MA Aina OO Ezechi OC Igwilo CI
author_facet	Ekama SO Ilomuanya MO Azubuike CP Bamidele TA Fowora MA Aina OO Ezechi OC Igwilo CI
author_sort	Ekama SO
title	Mucoadhesive Microspheres of Maraviroc and Tenofovir Designed for Pre-Exposure Prophylaxis of HIV-1: An in vitro Assessment of the Effect on Vaginal Lactic Acid Bacteria Microflora
title_short	Mucoadhesive Microspheres of Maraviroc and Tenofovir Designed for Pre-Exposure Prophylaxis of HIV-1: An in vitro Assessment of the Effect on Vaginal Lactic Acid Bacteria Microflora
title_full	Mucoadhesive Microspheres of Maraviroc and Tenofovir Designed for Pre-Exposure Prophylaxis of HIV-1: An in vitro Assessment of the Effect on Vaginal Lactic Acid Bacteria Microflora
title_fullStr	Mucoadhesive Microspheres of Maraviroc and Tenofovir Designed for Pre-Exposure Prophylaxis of HIV-1: An in vitro Assessment of the Effect on Vaginal Lactic Acid Bacteria Microflora
title_full_unstemmed	Mucoadhesive Microspheres of Maraviroc and Tenofovir Designed for Pre-Exposure Prophylaxis of HIV-1: An in vitro Assessment of the Effect on Vaginal Lactic Acid Bacteria Microflora
title_sort	mucoadhesive microspheres of maraviroc and tenofovir designed for pre-exposure prophylaxis of hiv-1: an in vitro assessment of the effect on vaginal lactic acid bacteria microflora
publisher	Dove Medical Press
publishDate	2021
url	https://doaj.org/article/ff1d6fe759434abfaea9640684009ac0
work_keys_str_mv	AT ekamaso mucoadhesivemicrospheresofmaravirocandtenofovirdesignedforpreexposureprophylaxisofhiv1aninvitroassessmentoftheeffectonvaginallacticacidbacteriamicroflora AT ilomuanyamo mucoadhesivemicrospheresofmaravirocandtenofovirdesignedforpreexposureprophylaxisofhiv1aninvitroassessmentoftheeffectonvaginallacticacidbacteriamicroflora AT azubuikecp mucoadhesivemicrospheresofmaravirocandtenofovirdesignedforpreexposureprophylaxisofhiv1aninvitroassessmentoftheeffectonvaginallacticacidbacteriamicroflora AT bamideleta mucoadhesivemicrospheresofmaravirocandtenofovirdesignedforpreexposureprophylaxisofhiv1aninvitroassessmentoftheeffectonvaginallacticacidbacteriamicroflora AT foworama mucoadhesivemicrospheresofmaravirocandtenofovirdesignedforpreexposureprophylaxisofhiv1aninvitroassessmentoftheeffectonvaginallacticacidbacteriamicroflora AT ainaoo mucoadhesivemicrospheresofmaravirocandtenofovirdesignedforpreexposureprophylaxisofhiv1aninvitroassessmentoftheeffectonvaginallacticacidbacteriamicroflora AT ezechioc mucoadhesivemicrospheresofmaravirocandtenofovirdesignedforpreexposureprophylaxisofhiv1aninvitroassessmentoftheeffectonvaginallacticacidbacteriamicroflora AT igwiloci mucoadhesivemicrospheresofmaravirocandtenofovirdesignedforpreexposureprophylaxisofhiv1aninvitroassessmentoftheeffectonvaginallacticacidbacteriamicroflora
_version_	1718391407208562688

Mucoadhesive Microspheres of Maraviroc and Tenofovir Designed for Pre-Exposure Prophylaxis of HIV-1: An in vitro Assessment of the Effect on Vaginal Lactic Acid Bacteria Microflora

Ejemplares similares