Carrageenan-Based Acyclovir Mucoadhesive Vaginal Tablets for Prevention of Genital Herpes

Women are the most affected by genital herpes, which is one of the most common sexually transmitted infections, affecting more than 400 million people worldwide. The application of vaginal microbicides could provide a safe method of protection. Acyclovir is a safe and effective medication for vaginal administration, and numerous benefits have been observed in the treatment of primary or recurrent lesions due to genital herpes. Vaginal tablets based on a combination of the polymers iota-carrageenan and hydroxypropyl methylcellulose were developed for the controlled release of acyclovir. Swelling, mucoadhesion and drug release studies were carried out in simulated vaginal fluid. The tablets, containing a combination of iota-carrageenan and hydroxypropyl methylcellulose, have an adequate uptake of the medium that allows them to develop the precise consistency and volume of gel for the controlled release of acyclovir. Its high mucoadhesive capacity also allows the formulation to remain in the vaginal area long enough to ensure the complete release of acyclovir. These promising formulations for the prevention of genital herpes deserve further evaluation.

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Safety_and_Pharmacokinetics_of_Dapivirine_Delivery.7

10.31234/osf.io/t4j95 ◽

2020 ◽

Author(s):

Lungwani Muungo

Keyword(s):

Adverse Events ◽

Hiv Transmission ◽

Plasma Concentrations ◽

Vaginal Fluid ◽

Time Curve ◽

Vaginal Microbicides ◽

Intravaginal Rings ◽

Lower Genital Tract ◽

The Matrix

Vaginal microbicides for the prevention of HIV transmission maybe an important option for protecting women from infection.Incorporation of dapivirine, a lead candidate nonnucleoside reversetranscriptase inhibitor, into intravaginal rings (IVRs) for sustainedmucosal delivery may increase microbicide product adherence andefficacy compared with conventional vaginal formulations. Twentyfourhealthy HIV-negative women 18–35 years of age were randomlyassigned (1:1:1) to dapivirine matrix IVR, dapivirine reservoir IVR,or placebo IVR. Dapivirine concentrations were measured in plasmaand vaginal fluid samples collected at sequential time points over the33-day study period (28 days of IVR use, 5 days of follow-up). Safetywas assessed by pelvic/colposcopic examinations, clinical laboratorytests, and adverse events. Both IVR types were safe and well toleratedwith similar adverse events observed in the placebo and dapivirinegroups. Dapivirine from both IVR types was successfully distributedthroughout the lower genital tract at concentrations over 4 logs greaterthan the EC50 against wild-type HIV-1 (LAI) in MT4 cells. Maximumconcentration (Cmax) and area under the concentration–time curve(AUC) values were significantly higher with the matrix than reservoirIVR. Mean plasma concentrations of dapivirine were ,2 ng/mL.These findings suggest that IVR delivery of microbicides is a viableoption meriting further study.Key Words: dapivirine, HIV, intravaginal ring, microbicide,pharmacokinetics, prevention

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Formulation and Evaluation of Nelfinavir Extended Release Trilayer Matrix Tablets by Design of Experiment

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2018.11.5.6 ◽

2018 ◽

Vol 11 (5) ◽

pp. 4259-4268

Author(s):

Nirmala Rangu ◽

Gande Suresh

Keyword(s):

Controlled Release ◽

Drug Release ◽

Hydroxypropyl Methylcellulose ◽

Magnesium Stearate ◽

Zero Order ◽

Matrix Tablets ◽

Drug Dissolution ◽

Crystalline Cellulose ◽

Dissolution Profile ◽

Release Formulation

The present study was aimed to develop once-daily controlled release trilayer matrix tablets of nelfinavir to achieve zero-order drug release for sustained plasma concentration. Nelfinavir trilayer matrix tablets were prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropyl methylcellulose (HPMC), PVP (Polyvinyl Pyrrolidine) K-30 and MCC (Micro Crystalline Cellulose). Barrier layers were prepared with Polyox WSR-303, Xanthan gum, microcrystalline cellulose and magnesium stearate. Based on the evaluation parameters, drug dissolution profile and release drug kinetics DF8 were found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (DF8) was described by the zero-order and best fitted to Higuchi model. FT-IR studies confirmed that there were no chemical interactions between drug and excipients used in the formulation. These results indicate that the approach used could lead to a successful development of a controlled release formulation of nelfinavir in the management of AIDS.

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Fabrication and In Vitro Evaluation of pH-Sensitive Polymeric Hydrogels as Controlled Release Carriers

Gels ◽

10.3390/gels7030110 ◽

2021 ◽

Vol 7 (3) ◽

pp. 110

Author(s):

Muhammad Suhail ◽

Chih-Wun Fang ◽

Arshad Khan ◽

Muhammad Usman Minhas ◽

Pao-Chu Wu

Keyword(s):

Controlled Release ◽

Drug Release ◽

Acrylic Acid ◽

Chondroitin Sulfate ◽

Diclofenac Sodium ◽

Research Work ◽

Controlled Delivery ◽

Scanning Calorimetry ◽

Release Studies

The purpose of the current investigation was to develop chondroitin sulfate/carbopol-co-poly(acrylic acid) (CS/CBP-co-PAA) hydrogels for controlled delivery of diclofenac sodium (DS). Different concentrations of polymers chondroitin sulfate (CS), carbopol 934 (CBP), and monomer acrylic acid (AA) were cross-linked by ethylene glycol dimethylacrylate (EGDMA) in the presence of ammonium peroxodisulfate (APS) (initiator). The fabricated hydrogels were characterized for further experiments. Characterizations such as Scanning electron microscopy (SEM), Thermogravimetric analysis (TGA), Differential scanning calorimetry (DSC), Powder X-ray diffractometry (PXRD), and Fourier transform infrared spectroscopy (FTIR) were conducted to understand the surface morphology, thermodynamic stability, crystallinity of the drug, ingredients, and developed hydrogels. The swelling and drug release studies were conducted at two different pH mediums (pH 1.2 and 7.4), and pH-dependent swelling and drug release was shown due to the presence of functional groups of both polymers and monomers; hence, greater swelling and drug release was observed at the higher pH (pH 7.4). The percent drug release of the developed system and commercially available product cataflam was compared and high controlled release of the drug from the developed system was observed at both low and high pH. The mechanism of drug release from the hydrogels followed Korsmeyer–Peppas model. Conclusively, the current research work demonstrated that the prepared hydrogel could be considered as a suitable candidate for controlled delivery of diclofenac sodium.

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Synthesis, characterization and drug release studies of poly(2-hydroxyethyl methacrylate)/KIT-5 nanocomposite as an innovative organic–inorganic hybrid carrier system

RSC Advances ◽

10.1039/c4ra13930e ◽

2015 ◽

Vol 5 (16) ◽

pp. 12463-12471 ◽

Cited By ~ 8

Author(s):

Roozbeh Javad Kalbasi ◽

Ali Zirakbash

Keyword(s):

Controlled Release ◽

Drug Release ◽

Hybrid Material ◽

Great Promise ◽

Hydroxyethyl Methacrylate ◽

Carrier System ◽

Inorganic Hybrid ◽

Drug Molecules ◽

System P ◽

Release Studies

PHEMA/KIT-5 with various pore sizes was prepared. Efficient encapsulation of drug molecules inside the pores of the hybrid material and controlled release of them in an aqueous medium, suggest the great promise of the composite as a carrier system.

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2017 European guidelines for the management of genital herpes

International Journal of STD & AIDS ◽

10.1177/0956462417727194 ◽

2017 ◽

Vol 28 (14) ◽

pp. 1366-1379 ◽

Cited By ~ 30

Author(s):

Rajul Patel ◽

Oliver J Kennedy ◽

Emily Clarke ◽

Anna Geretti ◽

Arvid Nilsen ◽

...

Keyword(s):

Genital Herpes ◽

Early Recognition ◽

Recurrent Genital Herpes ◽

Sexually Transmitted ◽

European Guidelines ◽

Duration Of Illness ◽

Clinical Scenarios ◽

Immunodeficiency Virus ◽

Initiation Of Therapy

Genital herpes is one of the commonest sexually transmitted infections worldwide. Using the best available evidence, this guideline recommends strategies for diagnosis, management, and follow-up of the condition as well as for minimising transmission. Early recognition and initiation of therapy is key and may reduce the duration of illness or avoid hospitalisation with complications, including urinary retention, meningism, or severe systemic illness. The guideline covers a range of common clinical scenarios, such as recurrent genital herpes, infection during pregnancy, and co-infection with human immunodeficiency virus.

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Suppressive valacyclovir therapy to reduce genital herpes transmission: Good public health policy?

McGill Journal of Medicine ◽

10.26443/mjm.v12i1.732 ◽

2020 ◽

Vol 12 (1) ◽

Author(s):

Paul E Bonnar

Keyword(s):

Genital Herpes ◽

Screening Program ◽

Antiviral Agent ◽

Suppressive Therapy ◽

Number Needed To Treat ◽

Economic Costs ◽

Transmitted Infection ◽

Herpes Simplex Viruses ◽

Sexually Transmitted ◽

Individual Level

Genital herpes is a widespread sexually transmitted infection caused by the herpes simplex viruses (HSV). Suppressive valacyclovir therapy has been shown to significantly reduce HSV transmission. The benefits and costs of using valacyclovir to reduce transmission in couples discordant for genital herpes will be analyzed in order to better inform decision-making. By reducing transmission, the physical and psychological harms of living with symptomatic genital herpes will be prevented while saving on certain healthcare costs. However, the large number needed to treat and the low symptomatic rate among infected individuals may outweigh these benefits. The costs of trying to achieve a significant reduction in incidence include the psychological harms of identifying asymptomatic individuals through a large screening program and the economic costs of the antiviral agent and screening. When these issues are weighed, the high economic costs render a program to reduce incidence unfeasible. Nevertheless, it is clinically important to consider the consequences of transmission at an individual level. The specific circumstances that influence the decision to use suppressive therapy are identified.

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FORMULATION DEVELOPMENT AND EVALUATION OF AN IN SITU OPHTHALMIC GELLING SYSTEM OF BRIMONIDINE TARTRATE AND TIMOLOL MALEATE FOR THE TREATMENT OF GLAUCOMA

INDIAN DRUGS ◽

10.53879/id.54.02.10854 ◽

2017 ◽

Vol 54 (02) ◽

pp. 76-78

Author(s):

A Shirodker ◽

◽

S. Bhangle ◽

R. Gude

Keyword(s):

Hydroxypropyl Methylcellulose ◽

In Vitro Release ◽

Content Uniformity ◽

Formulation Development ◽

Timolol Maleate ◽

Release Studies ◽

Brimonidine Tartrate ◽

In Situ Gelling

The present study involved formulation of an in situ gelling system of brimonidine tartrate and timolol maleate for the treatment of glaucoma. Carbopol® 980 NF, xanthum gum and hydroxypropyl methylcellulose K4 M were used as polymers. The prepared in situ gelling systems were evaluated for clarity, appearance, texture analysis, pH, viscosity, rheological properties, in vitro gelation, isotonicity, drug content uniformity, in vitro release studies, microbiological evaluation, ex vivo release studies and stability testing. The results of the attenuated total reflectance spectroscopy and differential scanning calorimetry studies confirmed that there is no incompatibility between the drugs and the excipients. The formulations exhibited pseudoplastic rheology and formulation 3 showed the highest release of both the drugs from the formulation. The stability studies showed that the formulation was stable over the given period of time. Thus, it is evident that the in situ gelling system is a promising drug delivery system for the treatment of glaucoma.

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The Role of Structural Gendered Racism in Effective Healthcare Utilization among Black American Women with Herpes Simplex Virus

Journal of Prevention and Health Promotion ◽

10.1177/26320770211049257 ◽

2021 ◽

pp. 263207702110492

Author(s):

Stephanie I. V. Cazeau-Bandoo ◽

Ivy K. Ho

Keyword(s):

Black Women ◽

Genital Herpes ◽

Healthcare Utilization ◽

Medical Providers ◽

Institutional Barriers ◽

Transmitted Infection ◽

Gendered Racism ◽

Sexually Transmitted ◽

Simplex Virus

The sexual health of Black women has been compromised by racial and discriminatory healthcare practices from slavery through current medical and institutional barriers to care. This paper proposes a conceptual framework that identifies the link between stigma, gendered racism, and historical underpinnings that contribute to ineffective healthcare utilization of Black women diagnosed with the chronic sexually transmitted infection (STI), genital herpes. This paper also draws attention to different social factors that act as barriers to effective healthcare utilization and influence the health outcomes of Black women beyond individual factors. Using a socio-ecological framework, this paper reviews multi-level (i.e., individual, interpersonal, community, and institutional/policy) influences of the experience of genital herpes among Black women. Recommendations are provided to improve the ability of health systems and medical providers to deliver appropriate services to diverse populations, thereby improving healthcare utilization and reducing disparities for Black women.

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Sexually transmitted infections

10.1093/med/9780198810858.003.0015 ◽

2021 ◽

pp. 603-628

Author(s):

Henrietta Williams

Keyword(s):

Human Papillomavirus ◽

Bacterial Vaginosis ◽

Sexually Transmitted Infections ◽

Genital Herpes ◽

Genital Warts ◽

Syndromic Management ◽

Sexually Transmitted ◽

Granuloma Inguinale ◽

Chlamydial Infections

Why are sexually-transmitted infections important??, Syndromic management of sexually-transmitted infections?, Syphilis?, Gonorrhoea?, Chlamydial infections?, Chancroid?, Granuloma inguinale donovanosis?, Trichomoniasis?, Bacterial vaginosis?, Genital herpes?, Candida vaginitis?, Human papillomavirus and genital warts?

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Chitosan-Based Mucoadhesive Vaginal Tablets for Controlled Release of the Anti-HIV Drug Tenofovir

Pharmaceutics ◽

10.3390/pharmaceutics11010020 ◽

2019 ◽

Vol 11 (1) ◽

pp. 20 ◽

Cited By ~ 19

Author(s):

Raúl Cazorla-Luna ◽

Fernando Notario-Pérez ◽

Araceli Martín-Illana ◽

Roberto Ruiz-Caro ◽

Aitana Tamayo ◽

...

Keyword(s):

Sexual Transmission ◽

Microstructural Characterization ◽

Vaginal Fluid ◽

Vaginal Mucosa ◽

Vaginal Microbicides ◽

Polyelectrolyte Complexes ◽

Antiretroviral Drug ◽

Sexual Transmission Of Hiv ◽

Self Protection

Vaginal microbicides have the potential to give women at high risk of contracting HIV the option of self-protection by preventing the sexual transmission of the virus. In this paper, mucoadhesive vaginal tablets based on chitosan, alone and in combination with pectin and locust bean gum, were developed for the sustained release of tenofovir (an antiretroviral drug). The formulations were placed in simulant vaginal fluid (SVF) to swell, and Hg porosity and SEM microscopy were used for the microstructural characterization of the swelling witnesses. The results show that the association of pectin and chitosan generated polyelectrolyte complexes and produced a robust system able to maintain its structure during the swelling process, when small pores are formed. Drug release and bovine vaginal mucoadhesion studies were performed in SVF showing that tenofovir-controlled dissolution profiles and adhesion to the mucosa were conditioned by the swelling processes of the polymer/s in each formulation. Tablets based on chitosan/pectin have the most homogeneous tenofovir dissolution profiles and last up to 96 h, remaining attached to the vaginal mucosa for the same period. These formulations can therefore be considered a good option for the self-protection of women from the sexual transmission of HIV.

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