Vaginal Delivery System Research Articles

Clinical Characteristics of the Controlled-Release Dinoprostone Vaginal Delivery System (PROPESS).

Clinical Characteristics of the Controlled-Release Dinoprostone Vaginal Delivery System (PROPESS).

Validation of spectrophotometric and colorimetric methods for determination of efavirenz in various biological matrices: Application to the development of dissolvable microneedle-based efavirenz complex inclusion for vaginal delivery

One of the antiretroviral treatments (ART) used to treat Human Immunodeficiency Virus (HIV) disease is efavirenz (EFV). EFV itself has bioavailability issues during oral therapy due to its poor solubility. When injected, administration issues arise. Hence, creating medication delivery methods was crucial to creating EFV delivery. HIV therapy benefits from the vaginal medication delivery system's ease of use, higher bioavailability, and quick systemic absorption in the surface folds. In this study, an inclusion complex (IC) was added to the EFV formulation to increase solubility, and dissolving microneedles (DMN) was used for delivery to increase penetration. Here, in support of this formulation creation process, we carried out validation utilizing spectrophotometric and colorimetric techniques. The amount of EFV was determined by validating ethanol and artificial vaginal fluid (AVF) using UV–Vis spectrophotometry. Vaginal tissue and plasma were also validated using colorimetric with the β-naphthol reagent. The International Council for Harmonization (ICH) and US Food and Drug Administration (FDA) requirements were adhered to in verifying the creation of analytical procedures. The outcomes demonstrated a linear correlation value of ≥0.9998. The LLOQ levels were 0.99 g/mL, 0.97 g/mL, 0.66 g/mL, 0.74 g/mL, and 0.74 g/mL in ethanol, AVF, porcine vaginal tissue, rat vaginal tissue, and vaginal plasma, respectively. The developed precision and accuracy were confirmed. The approach was successfully used to determine the amount of EFV in inclusion complex integration and DMN platform. The outcomes demonstrated high IC-EFV incorporation release and penetration profiles, permeation and high drug retention andex vivokinetics in the vagina and enhanced bioavailability fromin vivostudy pharmacokinetic profiles of DMN-IC-EFV.

Prospective study of pain levels when using controlled-release dinoprostone vaginal delivery system (PROPESS) compared with mechanical methods in pregnant women requiring cervical ripening

Prospective study of pain levels when using controlled-release dinoprostone vaginal delivery system (PROPESS) compared with mechanical methods in pregnant women requiring cervical ripening

Metronidazole loaded chitosan–phytic acid polyelectrolyte complex nanoparticles as mucoadhesive vaginal delivery system for bacterial vaginosis

Bacterial vaginosis (BV) is a recurring infection that is difficult to treat due to the limited bioavailability of antimicrobials. In this study, Metronidazole (MTZ)-loaded chitosan nanoparticles (MCSNP) were synthesized employing phytic acid (PA) as a crosslinking agent for treating bacterial vaginosis. The prepared MCSNPs were characterized for size, shape, surface charge, compatibility, cytotoxicity, biofilm inhibition, and in-vitro/in-vivo antimicrobial activities. Morphological examination revealed that nanoparticles generated from 0.535 % w/v chitosan and 0.112 % w/v PA were non-spherical, discontinuous, and irregular, with zeta potential ranging from 25.00 ± 0.45 to 39 ± 0.7. The results of DSC and XRD demonstrated no change in the physical state of the drug in the finished formulation. The optimized formulation demonstrates a cumulative drug release of about 98 ± 1.5 % within 8 h. Antimicrobial studies demonstrated that the optimized formulation had enhanced efficacy against acid-adapted BV pathogens, with a MIC value of 0.9 ± 0.1 μg/mL. Compared to the MTZ alone, the in-vivo antibacterial results of in the case of developed nanoparticles showed a four-fold reduction in bacterial count in female Swiss albino mice. Based on the experimental findings, it was concluded that MCSNPs, due to their excellent physiochemical and antibacterial properties, could serve as a potential topical alternative for treating BV.

A Retrospective Comparative Study of the Effect of Controlled-Release Dinoprostone Vaginal Delivery System (Propess®) and Mechanical Methods for Cervical Ripening in Nulliparous Women in Late-Term Pregnancy.

The effects of the controlled-release dinoprostone vaginal delivery system (Propess®) and mechanical methods for cervical ripening in nulliparous women in late-term pregnancy were compared retrospectively. This retrospective comparative study included 46 nulliparous pregnant women (24 in the Propess®group and 22 in the mechanical methods groups) with a low Bishop score (≤1) who needed labor induction at 41 weeks of gestation. The primary outcome was the success rate of cervical ripening (= Bishop score >6 or vaginal delivery) by the next day following the insertion of Propess®only or mechanical cervical dilation only. In the cases in which cervical ripening was unsuccessful, other methods were performed, and the success rate of cervical ripening the day after was compared as the secondary outcome. As the primary outcome, there was not a significant difference in the success rate of cervical ripening between the Propess®and mechanical methods groups (21 vs. 22%, p = 0.88). As for the secondary outcomes, there was not a significant difference in the total success rate of cervical ripening between the two groups (75 (5+13/24) vs. 73 (5+11/22)%, p = 0.86)). Of the unsuccessful cervical ripening cases as secondary outcomes, the Bishop score of all was ≤2 on the second day of hospitalization. The combined use of Propess®and mechanical methods was effective for cervical ripening in nulliparous women with a low Bishop score in late-term pregnancy, regardless of order.

Comparison of Obstetric Outcomes Between Controlled-Release Dinoprostone Vaginal Delivery System (PROPESS) and Administration of Oral Dinoprostone for Labor Induction in Multiparous Women at Term.

The aim of this study was to compare the rate of vaginal delivery and adverse outcomes of a controlled-release dinoprostone vaginal delivery system (PROPESS) and the administration of oral dinoprostone for labor induction in multiparous women at term. This retrospective case-controlled study included 92 multiparous pregnant women (46 and 46 in the PROPESS and oral dinoprostone groups, respectively) who required labor induction at ≥37 weeks of gestation. The primary outcome was the success rate of vaginal delivery following the insertion of PROPESS only or the administration of oral dinoprostone (up to six tablets) only. The secondary outcomes were uterine tachysystole with non-reassuring fetal status, the proportion of cases requiring pre-delivery oxytocin, and the rate of cesarean delivery. The proportion of pregnant women who delivered vaginally as the primary outcome was significantly higher in the PROPESS group (33/46 [72%]) than in the oral dinoprostone group (16/46 [35%], p < 0.01). In the secondary outcomes, the proportion of cases requiring pre-delivery oxytocin in the PROPESS group was significantly lower than that in the oral dinoprostone group (24% vs. 57%, p < 0.01). In multiparous women at term, PROPESS may be able to induce labor and lead to a higher vaginal delivery rate without adverse outcomes compared to oral dinoprostone.

Prediction of an effective cervical ripenning in the induction of labour using vaginal dinoprostone

To develop a predictive model for successful cervical ripening in women that undergo induction of labour by means of a vaginal prostaglandin slow-release delivery system (Propess®). Prospective observational study on 204 women that required induction of labour between February 2019 and May 2020 at “La Mancha Centro” hospital in Alcázar de San Juan, Spain. The main variable studied was effective cervical ripening (Bishop score > 6). Using multivariate analysis and binary logistic regression, we created three initial predictive models (model A: Bishop Score + Ultrasound cervical length + clinical variables (estimated fetal weight, premature rupture of membranes and body mass index)); model B: Ultrasound cervical lenght + clinical variables; and model C: Bishop score + clinical variables) to predict effective cervical ripening. All three predictive models obtained (A, B and C) presented good predictive capabilities, with an area under the ROC curve ≥ 0.76. Predictive model C, composed of the variables: gestational age (OR 1.55, 95% CI 1.18–2.03, p = 0.002), premature rupture of membranes (OR 3.21 95% CI 1.34–7.70, p = 0.09) body mass index (OR 0.93, 95% CI 0.87–0.98, p = 0.012), estimated fetal weight (OR 0.99, 95% CI 0.99–1.00, p = 0.068) and Bishop score (OR 1.49 95% CI 1.18–1.81, p = 0.001), is presented as the model of choice with an area under the ROC curve of 0.76 (95% CI 0.70–0.83, p < 0.001). A predictive model composed of the variables: gestational age, premature rupture of membranes, body mass index, estimated fetal weight and Bishop score upon admission presents good capabilities in predicting successful cervical ripening following administration of prostaglandins. This tool could be useful in making clinical decisions with regard to induction of labour.

In-Vitro Dissolution Study protocol for various Vaginal Dosage Forms

The vaginal mucosa is well recognized as a route for delivering variety of drugs. Considerable number of anti-fertility drugs have been successfully delivered through vaginal and uterine canals. The goal of this review is to summarize the present clinical state of intravaginal medicines and IUDs, with a prime focus on the available in-vitro dissolution study methods and their importance. At present different vaginal drug delivery systems are available in the market and a few are under clinical trial. The accurate estimation drug release profile of any of such dosage form is primarily depends on the standard dissolution study protocol. The vaginal delivery system is an effective site for local and systemic drug delivery, and a range of innovative formulation strategies are being researched for its development. The concept behind the study is mainly lies on the fact that the standard dissolution protocol may vary based on formulation type, its design and its therapeutic goals.

Overview of Emulgel as Emergent Topical Delivery: Recent Applications and Advancement

Emulgel is an emerging delivery system with added advantages over other topical delivery systems which is proven to be boon for cosmetics and dermatology. Emulgels are emulsion which is converted to Gel, which will make it a non greasy and enhances patient compliance. The amalgamation of the two systems would be advantages in term of high drug loading capacity and low skin irritation, site specific targeting avoiding first-pass metabolism and increase in bioavailability. Work carried out by researchers proved that, Emulgel/ Nanoemulgel loaded with drugs has been found effective in many topical disorders and it is emerging as potential drug delivery system in area of dermatology. In the present review current research works that carried out on Emulgel and nano emulgels are discussed and also highlighted the recent applications of Emulgel in transdermal as well as dental, ocular, vaginal, and other delivery system.

Engineering of Vaginal Lactobacilli to Express Fluorescent Proteins Enables the Analysis of Their Mixture in Nanofibers.

Lactobacilli are a promising natural tool against vaginal dysbiosis and infections. However, new local delivery systems and additional knowledge about their distribution and mechanism of action would contribute to the development of effective medicine. This will be facilitated by the introduction of the techniques for effective, inexpensive, and real-time tracking of these probiotics following their release. Here, we engineered three model vaginal lactobacilli (Lactobacillus crispatus ATCC 33820, Lactobacillus gasseri ATCC 33323, and Lactobacillus jensenii ATCC 25258) and a control Lactobacillus plantarum ATCC 8014 to express fluorescent proteins with different spectral properties, including infrared fluorescent protein (IRFP), green fluorescent protein (GFP), red fluorescent protein (mCherry), and blue fluorescent protein (mTagBFP2). The expression of these fluorescent proteins differed between the Lactobacillus species and enabled quantification and discrimination between lactobacilli, with the longer wavelength fluorescent proteins showing superior resolving power. Each Lactobacillus strain was labeled with an individual fluorescent protein and incorporated into poly (ethylene oxide) nanofibers using electrospinning, as confirmed by fluorescence and scanning electron microscopy. The lactobacilli retained their fluorescence in nanofibers, as well as after nanofiber dissolution. To summarize, vaginal lactobacilli were incorporated into electrospun nanofibers to provide a potential solid vaginal delivery system, and the fluorescent proteins were introduced to distinguish between them and allow their tracking in the future probiotic-delivery studies.

Formulation and Evaluation of Vaginal Bioadhesive Drug Delivery System of Acyclovir

Acyclovir is an anti-viral, which has been used in the treatment of vaginal disorder. Acyclovir is almost completely absorbed after oral administration but has low bioavailability of about 10-15% because of first pass metabolism. As first pass metabolism removes approximately 85-90% of the drug, so for clinical efficacy of the drug it should be frequently administered. Hence an attempt has been made to produce sustained release dosage form of the acyclovir which can be specifically employed for the treatment of vaginal disordered by Herpes simplex virus. The Mucoadhesive tablets of acyclovir has been prepared by direct compression methods and evaluated for various parameter such as thickness, friability, hardness, drug content, weight variation, swelling index, surface pH, bioadhesive force, bioadhesive time, drug release etc. The kinetic data was applied to the optimized formulations. So formulation of acyclovir in a vaginal mucoadhesive tablet dosage form will decrease the frequency of administration, which can lead to an improvement in patient adherence and thereby improving its clinical efficacy.

Comparison of perinatal outcomes between controlled-release dinoprostone vaginal delivery system (PROPESS) and metreurynter for cervical ripening in labor induction: A retrospective single-center study in Japan.

This study aimed to compare the efficacy and safety of a controlled-release dinoprostone vaginal delivery system (PROPESS) and a metreurynter for labor induction. This retrospective case-controlled study included 117 pregnant women (51 and 66 in the PROPESS and metreurynter groups, respectively) who required labor induction after >37 weeks' gestation at Mie University Hospital between January 2018 and September 2020. The primary outcome was the success rate of vaginal delivery. The secondary outcomes were changes in the Bishop score from the first insertion of PROPESS or the metreurynter to removal, uterine hyperstimulation and non-reassuring fetal status during the first insertion, proportion of pregnant women who needed pre-delivery oxytocin after removal, time to vaginal delivery after the first insertion, proportion of pregnant women who delivered vaginally within 12 or 24 h after the first insertion, and neonatal outcomes. The proportion of pregnant women, especially primiparas, who delivered vaginally was significantly higher in the PROPESS group (26/34 [76.5%]) than in the metreurynter group (25/52 [48.1%]; p=0.01). Moreover, among multiparas in the PROPESS group who delivered vaginally, nine (56.3%) out of 16 women delivered vaginally within 3h of labor onset. PROPESS for cervical ripening may reduce the risk of undergoing cesarean section in pregnant women requiring labor induction, especially primiparas. It is important to consider the possibility of precipitate labor when using the PROPESS in multiparas.

Physicochemical evaluation and pharmacodynamics of itraconazole-loaded liquid crystal precursor for vaginal delivery

Purpose To develop a liquid crystal (LC) precursor that can be used as a novel vaginal delivery system for Itraconazole (ITZ) and evaluate its pharmacodynamics. Methods The LC precursor was prepared by using phytantriol (PYT) as lipid matrix and N, N-dimethylformamide (DMAC) as solvent. Swelling studies were performed to assess the phase conversion ability. The formulations were characterized by crossed polarized light microscopy (CPLM), small-angle X-ray scattering (SAXS). Moreover, the rheological and in vitro drug release behavior were investigated. Then the vaginal retention time of ITZ in the optimal prescription was evaluated. Finally, the pharmacodynamics studies of the ITZ-loaded LC precursor were performed in a mouse model of vulvovaginal candidiasis (VVC). Results The LC precursor could transform to LC gels after administration into the vagina. Based on PLM and SAXS, the LC gels, formed after phase-conversion, were cubic LC. The LC precursor was non-Newtonian, while the LC gels exhibited a pseudo-plastic fluid behavior. In vitro release results revealed that F2 (68.0%) had a higher cumulative drug release than that of F1 (59.17%) at 72 h. Most of the LC gels could be retained in the vagina of mice for 24–36 h. Pharmacodynamics studies showed that there was only mild inflammation or no inflammatory stimulation in the control group. The ITZ-loaded LC precursor significantly improved the symptoms of vaginitis in mice and had a better therapeutic effect than that of the positive control group. Conclusions The ITZ-loaded LC precursor would be a promising formulation for vaginal drug delivery.

A Survey on Mucoadhesive Thermoreversible Drug Delivery System with special Emphasis on Recto-Anal Region for the Treatment of Internal Hemorrhoids

The concept of combination of thermo reversibility and mucoadhesion has achieved a much valuable interest in various fields of pharmaceutics. Mucoadhesive drug delivery systems interact with the mucus layer covering the mucosal epithelial surface, and mucin molecules and increase the residence time of the dosage form at the site of absorption. Thermoreversible gels are the hydrogels that are liquids at room temperature but undergo gelation when in contact with body fluids or change in pH. A major problem faced by conventional formulation in various routes of administration viz. nasal, ocular, vaginal, rectal, etc is drainage of instilled formulation, poor patient compliance as in the case of vaginal and rectal delivery system. Also, blurred vision and irritation to mucosa is observed in the case of ocular and nasal delivery respectively. The drainage of the formulation results in inaccurate dose delivery thus decreasing the bioavailability of the drug which demands an increase in the frequency of the administration. To overcome these limitations, there is need of novel delivery system such as thermoreversible mucoadhesive insitu gel which provides an ease of administration and improved patient compliance as these smart delivery system is free flowing liquid at ambient temperature and gels at physiological temperature which is higher than the LCST (low critical solution temperature) of thermoreversible polymer. The combined effect of mucoadhesion and thermoreversible property will enhance prolongation of residence time of dosage form and the accuracy of the dose in body cavity respectively, leading to increased bioavailability of the drug. This review focuses on benefits of mucoadhesive thermoreversible system of drug delivery through rectum for the treatment of internal hemorrhoids.

CURCUMIN LOADED POLYMERIC MICROSPHERES FOR VAGINAL DELIVERY: FORMULATION DESIGN, IN VITRO EVALUATION, KINETICS AND STABILITY STUDIES

The main objective of this research is to evaluate a new approach for the preparation of bio adhesive microparticles and to design an innovative vaginal delivery system for curcumin which is able to enhance the drug anticancer activity. Curcumin encapsulated microspheres were prepared by solvent evaporation method. The microspheres were found to be discrete, spherical with free-flowing properties and evaluated for particle size analysis, shape (scanning electron microscopy), drug encapsulation efficiency, FTIR, DSC studies and in vitro release performance. The best selected microsphere formulation (F2, containing drug: polymer ratio 1:2) was incorporated into gels with a bio adhesive polymer. The microencapsulated vaginal gels were evaluated for pH, spreadability, extrudability, viscosity, in vitro drug release, drug release kinetics, bio adhesion test, accelerated stability of selected gel formulation. In vitro drug release rate for selected microencapsulated bio adhesive vaginal gel (FS3 gel, containing 1 % w/w of drug loaded microspheres and 0.6 % w/w of Carbopol 934) was found to sustain curcumin over 12h. The results were then compared statistically and obtained a satisfactory correlation. Thus, in conclusion preparation protocol of microencapsulated vaginal gel study may be adopted for a successful development of newer drug delivery system of other drugs for administration to vagina.

Tailoring thixotropic mixed-lipid nanoconstructs of voriconazole for the management of Vulvovaginal candidiasis: Formulation, statistical optimization, in vitro characterization and in vivo assessment

Vulvovaginal candidiasis is a pervasive gynecological condition among women worldwide due to infection recurrence and resistance to conventional drugs. This calls for a novel formulation of alternative medication and with enhanced efficacy. This study aimed to fabricate mixed-lipid nanoconstructs (MLNCs) of voriconazole (VCZ) with a low concentration of lipids applying high shear homogenization and ultrasonication to form a semisolid formulation. Tefose 63 and Gelot 64 were employed as emulsifiers that are specified for vaginal preparations; as per their mucoadhesive properties and their texture enhancing characters, although usually used as lipids in different lipid carriers. A 24 factorial design was established and the optimized formulation was prepared using 10% total lipids, in which solid lipids (Sterotex NF: Glyceryl monostearate) ratio was 1.92:1 and the oils percentage was 30% (Maisine: Glyceryl monooleate, in the ratio of 1:1), and the emulsifiers mixture (Tefose 63: Gelot 64) ratio was 1:1, as 10% of total formulation weight. The optimized formulation with a viscosity of 964.49 ± 57.99 cp showed spherical nanoparticles (322.72 ± 15.11 nm) that entrapped 67.16 ± 3.45% of VCZ and exhibited release of 70.08 ± 2.87% in 8 h. The optimized formulation with high bioadhesive potentials significantly reduced the fungal burden in female Wistar rats infected with vaginal candidiasis, compared to the aqueous VCZ suspension (p < .05). Furthermore, in vivo histopathological findings proved the effectiveness and the safety of the optimized MLNCs formulation after vaginal application. Inclusively, MLNCs formulation could be a promising vaginal delivery system of VCZ for the treatment of vulvovaginal candidiasis.

Elution from intact and broken vaginal contraceptive rings: an in vitro study.

The in vitro elution of the active substances etonogestrel (ETO) and ethinylestradiol (EE) of Ornibel® (a vaginal delivery system) was determined after a deliberate breakage of the vaginal contraceptive ring and compared to the standard elution and hormone release of intact rings under the same experimental conditions. Ornibel® intact and broken vaginal rings were placed in a dissolution buffer and subject to a repetitive sampling of ETO and EE following a standardized in vitro elution (IVE) procedure for 21 days. The hormone dissolution profile was determined by HPLC using a fully validated analytical method. In a second study, rings were broken after day seven, and their elution profiles were compared to that of intact rings. For all utilized batches, the stability conditions established were 24 months at 5°C. Furthermore, no special storage conditions are needed. The instantaneous elution on day 1 of ETO and EE for intact rings were 119±8 µg/day and 15±1 µg/day, respectively (mean ± SD), which was non-significantly different to the immediate release of ETO and EE for broken rings (118±4 µg/day and 14±1 µg/day). The average elution profile for days 2-20 were 132±5 µg/day and 18±1 µg/day (ETO/EE, intact rings) and 132±4 µg/day and 19±1 µg/day (ETO/EE, broken rings) respectively. On day 21, the elution of ETO and EE was numerically similar 111±5 (±4) µg/day and 18±1 µg/day) for both intact and broken rings. The IVE results from intact rings and vaginal rings deliberately cut on day seven similarly did not differ in their release of ETO and EE. Our study concludes that the hormonal release of ETO and EE from Ornibel® are similar for intact and broken vaginal rings under standardized in vitro conditions.

Evaluation of polycaprolactone matrices for sustained intravaginal delivery of a natural macromolecular microbicide, lactoferrin

Polycaprolactone (PCL) matrices incorporating lactoferrin as a natural macromolecular microbicide, were prepared by rapidly cooling a suspension of lactoferrin particulates in PCL solution to induce crystallisation and hardening of the polymer. Thermal analysis revealed a 7% decrease in crystallinity of the PCL phase for 10% lactoferrin-loaded matrices compared with lactoferrin-free matrices and a 41% decrease in hardness of lactoferrin -loaded matrices, indicating a major influence of lactoferrin through inhibition of PCL crystal nucleation and growth. Exposure of the matrices to simulated vaginal fluid (SVF) at 37 °C resulted in rapid release of 13–14% of the lactoferrin content on day 1 and sustained delivery of the glycoprotein with high efficiency (90–95% of the content) over 14 days. SDS-PAGE analysis confirmed molecular weight preservation of the lactoferrin released from PCL matrices into SVF, indicating that it was not degraded during formulation and release. These findings recommend further investigations of PCL matrices as vaginal delivery systems for controlled release of macromolecular microbicides in the treatment and prevention of sexually transmitted infections.

Localized Therapy of Vaginal Infections and Inflammation: Liposomes-In-Hydrogel Delivery System for Polyphenols

Natural polyphenols, such as resveratrol (RES) or epicatechin (EPI), are attractive for treatments of various diseases, including vaginal infections and inflammation, because of their strong anti-oxidative and anti-inflammatory properties. However, their low solubility and consequent poor bioavailability limit their therapeutic uses. To overcome these limitations, a vaginal delivery system comprising either RES or EPI liposomes-in-hydrogel was developed. This system permits therapeutic action of both liposomal polyphenol (RES or EPI) and chitosan-based hydrogel. Liposomes of around 200 nm and entrapment efficiency of 81% and 77% for RES and EPI, respectively, were incorporated into chitosan hydrogel, respectively. Medium molecular weight chitosan (2.5%, w/w) was found to have optimal texture properties and mucoadhesiveness in ex vivo conditions. The in vitro release studies confirmed the sustained release of polyphenols from the system. Both liposomal polyphenols and polyphenols-in-liposomes-in-hydrogel exhibited only minor effects on cell toxicity. EPI showed superior radical scavenging activity at lower concentrations compared to antioxidants vitamin C and E. Anti-inflammatory activity expressed as the inhibitory activity of formulations on the NO production in the LPS-induced macrophages (RAW 264.7) confirmed the superiority of EPI liposomes-in-hydrogel. The plain liposomes-in-hydrogel also exhibited potent anti-inflammatory activity, suggesting that chitosan hydrogel acts in synergy regarding anti-inflammatory effect of formulation.

Preclinical Safety Evaluation of HIV-1 gp120 Responsive Microbicide Delivery System in C57BL/6 Female Mice.

Many novel vaginal/rectal microbicide formulations failed clinically due to safety concerns, indicating the need for the early investigation of lead microbicide formulations. In this study, the preclinical safety of an HIV-1 gp120 and mannose responsive microbicide delivery system (MRP) is evaluated in C57BL/6 mice. MRP was engineered through the layer-by-layer coating of calcium carbonate (CaCO3) with Canavalia ensiformis lectin (Con A) and glycogen. MRP mean particle diameter and zeta potential were 857.8 ± 93.1 nm and 2.37 ± 4.12 mV, respectively. Tenofovir (TFV) encapsulation and loading efficiencies in MRP were 70.1% and 16.3% w/w, respectively. When exposed to HIV-1 rgp120 (25 μg/mL), MRP released a significant amount of TFV (∼5-fold higher) in vaginal and seminal fluid mixture compared to the control (pre-exposure) level (∼59 μg/mL) in vaginal fluid alone. Unlike the positive control treated groups (e.g., nonoxynol-9), no significant histological damages and CD45+ cells infiltration were observed in the vaginal and major reproductive organ epithelial layers. This was probably due to MRP biocompatibility and its isosmolality (304.33 ± 0.58 mOsm/kg). Furthermore, compared to negative controls, there was no statistically significant increase in pro-inflammatory cytokines such as IL1α, Ilβ, IL7, IP10, and TNFα. Collectively, these data suggest that MRP is a relatively safe nanotemplate for HIV-1 gp120 stimuli responsive vaginal microbicide delivery system.