Microbicide vaginal rings: Technological challenges and clinical development

Malcolm, R. Karl; Boyd, Peter; McCoy, Clare; Murphy, Diarmaid J.

doi:10.1016/j.addr.2016.01.015

Cited by 90 publications

(118 citation statements)

References 222 publications

(354 reference statements)

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“…Despite significant progress in recent decades, human immunodeficiency virus type 1 (HIV‐1)/acquired immunodeficiency syndrome (AIDS) is still the leading cause of mortality among adults aged 15–59 years old and women in sub‐Saharan Africa bear the disproportionate share of this disease burden . A current focus of product developers includes the use of microbicides for HIV pre‐exposure prophylaxis (PrEP) that women can self‐administer to reduce the risk of infection . Strategies for delivery of microbicides for HIV PrEP include the use of topical gels, films, daily dosing via oral pills, and long‐acting vaginal rings (VRs) .…”

Section: Introductionmentioning

confidence: 99%

“…A current focus of product developers includes the use of microbicides for HIV pre‐exposure prophylaxis (PrEP) that women can self‐administer to reduce the risk of infection . Strategies for delivery of microbicides for HIV PrEP include the use of topical gels, films, daily dosing via oral pills, and long‐acting vaginal rings (VRs) . However, adherence to these strategies are not absolute .…”

Section: Introductionmentioning

confidence: 99%

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Design, Formulation, and Evaluation of Novel Dissolving Microarray Patches Containing Rilpivirine for Intravaginal Delivery

Crudden

Larrañeta

Clark

et al. 2019

Adv Healthcare Materials

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Antiretroviral (ARV) drugs have, for many years, been studied and administered in the prevention and treatment of human immunodeficiency virus (HIV). Intramuscular (IM) injection of long acting (LA) ARVs are in clinical development, but injectable formulations require regular access to healthcare facilities and disposal facilities for sharps. The development of a discrete, self‐administered, and self‐disabling vehicle to deliver ARVs could obviate these issues. This study describes the formulation, mechanical characterization, and in vivo evaluation of dissolving microarray patches (MAPs) containing a LA nanosuspension of the ARV, rilpivirine (RPV, RPV LA), for vaginal delivery. This is the first study to apply MAPs into vaginal tissue. The RPV LA MAPs penetrate ex vivo skin and a synthetic vaginal skin model and withstand the effects of potential dragging motion across synthetic vaginal epithelium. In in vivo studies, the mean plasma concentration of RPV in rats at the 56 day endpoint (116.5 ng mL−1) is comparable to that achieved in the IM control cohort (118.9 ng mL−1). RPV is detected systemically, in lymph and vaginal tissue, indicating the potential to deliver RPV LA to primary sites of viral challenge and replication. This innovative research has future potential for patients and healthcare workers, particularly in low‐resource settings.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Design, Formulation, and Evaluation of Novel Dissolving Microarray Patches Containing Rilpivirine for Intravaginal Delivery

Crudden

Larrañeta

Clark

et al. 2019

Adv Healthcare Materials

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“…Progestinski vaginalni prstenovi, subdermalni (supkutani) implanti i IUS sadrže samo progestinsku komponentu (progesteron, levonorgestrel, etonogestrel, nestoron) i mogu ih koristiti: porodilje koje aktivno doje (najmanje 4 puta dnevno) i žene sa faktorima rizika za upotrebu KHK (pušenje, više od 35 godina, hipertenzija) ili kontraindikacijama za upotrebu egzogenog estrogena [7,41,47,54,55].…”

Section: Terapijski Sistemi Za Progestinsku Kontracepcijuunclassified

“…Supstanca je homogeno dispergovana u matriksu silikonskog elastomera. Registrovan je pod imenom Progering  (Laboratorio Silesia SA, Čile i Andromaco SA, Argentina) na tržištu nekih zemalja Latinske Amerike (Čile, Peru, Bolivija, Dominikanska Republika, Ekvador, Gvatemala, Panama, Ekvador i Honduras) [41,47], a od 2015. godine svrstan je na listu osnovnih lekova koju predlaže SZO. Aktivna supstanca se oslobađa prosečnom brzinom od 10 mg/24 h tokom 90 dana.…”

Section: Vaginalni Prstenovi Za Progestinsku Kontracepcijuunclassified

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Pharmaceutical-technological aspects of therapeutic systems for hormonal contraception

Djekić¹,

Primorac²

2016

Arh farmaciju

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Univerzitet u Beogradu -Farmaceutski fakultet, Katedra za farmaceutsku tehnologiju i kozmetologiju, Vojvode Stepe 450, 11221 Beograd, Srbija Kratak sadržajUpotreba terapijskih sistema za hormonsku kontracepciju (TSHK) predstavlja značajan alternativni vid sprečavanja neplanirane trudnoće u odnosu na primenu hormonskih kontraceptiva per os, pri čemu se otklanja rizik od gastrointestinalnih neželjenih reakcija, omogućava smanjenje terapijske doze, učestalosti primene i sistemskih neželjenih dejstava i povećava nivo adherence. Do sada su razvijeni terapijski sistemi tipa transdermalnih flastera, subdermalnih (supkutanih) implanata, vaginalnih prstenova i intrauternih terapijskih (dostavnih) sistema (IUS) za hormonsku kontracepciju progestinima (progesteron, levonorgestrel, etonogestrel, nestoron) ili kombinacijama progestina i estrogena (norelgestormin + etinilestradiol, gestoden + etinilestradiol, etonogestrel + etinilestradiol, levonorgestrel + etinilestradiol, nestoron + etinilestradiol, nestoron + estradiol). U radu su prikazane glavne karakteristike navedenih tipova TSHK, kao i specifičnosti farmaceutskih proizvoda ove vrste u pogledu sastava i primene. Opisani su glavni mehanizmi za postizanje kontrolisanog produženog oslobađanja hormona i efikasnost za isporuku aktivnih supstanci kod različitih TSHK. Predstavljeni su najznačajniji savremeni pristupi u dizajnu terapijskih sistema ove vrste sa ciljem da se pojednostavi njihova primena, poboljša podnošljivost, prihvatljivost i terapijska efikasnost, a ukazano je i na mogućnost korišćenja novih tehnologija u razvoju terapijskih sistema za višenamensku prevenciju začeća i infekcije virusom humane imunodeficijencije (human immunodeficiency virus, HIV).Ključne reči: terapijski sistemi za hormonsku kontracepciju; transdermalni flaster; subdermalni (supkutani) implant; vaginalni prsten; intrauterini terapijski (dostavni) sistem; progestini; estrogeni; kontrolisano/produženo oslobađanje; tehnologije za višenamensku prevenciju.

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Controlled Drug Delivery via the Vaginal and Rectal Routes

Neves

Sarmento

2021

Fundamentals of Drug Delivery

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Microbicide vaginal rings: Technological challenges and clinical development

Cited by 90 publications

References 222 publications

Design, Formulation, and Evaluation of Novel Dissolving Microarray Patches Containing Rilpivirine for Intravaginal Delivery

Design, Formulation, and Evaluation of Novel Dissolving Microarray Patches Containing Rilpivirine for Intravaginal Delivery

Pharmaceutical-technological aspects of therapeutic systems for hormonal contraception

Controlled Drug Delivery via the Vaginal and Rectal Routes

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