Rational Development of Liposomal Hydrogels: A Strategy for Topical Vaginal Antiretroviral Drug Delivery in the Context of HIV Prevention

Faria, Maria João; Machado, Raúl; Ribeiro, Artur; Gonçalves, Hugo; Oliveira, M. Elisabete; Viseu, Teresa; Neves, José das; Lúcio, Marlene

doi:10.3390/pharmaceutics11090485

Cited by 41 publications

(28 citation statements)

References 75 publications

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“…Other reports showed similar findings where the dispersion of vesicular carriers into various gel bases resulted in reduced drug release rates [62,63]. It is believed that drug release from vesicles suspended in gel bases occurs through two steps; drug release from the vesicles, which act as a drug reservoir followed by diffusion through the gel network [64]. The presence of the gel network results in an increased diffusion path and subsequent reduction in drug release rate.…”

Section: In Vitro Drug Release Studiesmentioning

confidence: 62%

Liposomal and Ethosomal Gels for the Topical Delivery of Anthralin: Preparation, Comparative Evaluation and Clinical Assessment in Psoriatic Patients

2020

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To enhance anthralin efficacy against psoriasis and reduce its notorious side effects, it was loaded into various liposomal and ethosomal preparations. The nanocarriers were characterized for drug encapsulation efficiency, size, morphology and compatibility between various components. Optimum formulations were dispersed in various gel bases and drug release kinetics were studied. Clinical efficacy and safety of liposomal and ethosomal Pluronic®F-127 gels were evaluated in patients having psoriasis (clinicaltrials.gov identifier is NCT03348462). Safety was assessed by recording various adverse events. Drug encapsulation efficiency ≥97.2% and ≥77% were obtained for liposomes and ethosomes, respectively. Particle sizes of 116 to 199 nm and 146 to 381 nm were observed for liposomes and ethosomes, respectively. Fourier-Transform infrared (FT-IR) spectroscopy and differential scanning calorimetry (DSC) studies confirmed the absence of interaction between anthralin and various nanocarrier components. Tested gel bases showed excellent ability to sustain drug release. At baseline, the patients had a median Psoriasis Area and Severity Index (PASI) of 3.4 for liposomes and 3.6 for ethosomes without significant difference. After treatment, mean PASI change was −68.66% and −81.84% for liposomes and ethosomes, respectively with a significant difference in favor of ethosomes. No adverse effects were detected in both groups. Anthralin ethosomes could be considered as a potential treatment of psoriasis.

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Section: In Vitro Drug Release Studiesmentioning

confidence: 62%

Liposomal and Ethosomal Gels for the Topical Delivery of Anthralin: Preparation, Comparative Evaluation and Clinical Assessment in Psoriatic Patients

2020

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“…The potential of PEG-400 has been studied extensively in solubility enhancement of various drugs [9][10][11][12][13][14][15][16][17][18]. Several formulation approaches including "3D printed controlled release tablets [4], film coated tablets [19], rapidly disintegrating vaginal tablets [20], immediate release tablets [21], vaginal gels [22], liposomal gels [23], microparticulate drug delivery system [24], nanosuspensions [25,26] and polymeric nanoparticles [5,27,28]" were reported to improve antiviral therapy and pharmacokinetic profile of ECT. The equilibrium solubility of ECT in water was found as 112 mg mL −1 at "T = 298.2 K" [1].…”

Section: Introductionmentioning

confidence: 99%

Solubility, Hansen Solubility Parameters and Thermodynamic Behavior of Emtricitabine in Various (Polyethylene Glycol-400 + Water) Mixtures: Computational Modeling and Thermodynamics

2020

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This study was aimed to find out the solubility, thermodynamic behavior, Hansen solubility parameters and molecular interactions of an antiviral drug emtricitabine (ECT) in various “[polyethylene glycol-400 (PEG-400) + water]” mixtures. The solubility of ECT in mole fraction was determined at “T = 298.2 to 318.2 K” and “p = 0.1 MPa” using an isothermal method. The experimental solubilities of ECT in mole fraction were validated and correlated using various computational models which includes “Van’t Hoff, Apelblat, Yalkowsky-Roseman, Jouyban-Acree and Jouyban-Acree-Van’t Hoff models”. All the models performed well in terms of model correlation. The solubility of ECT was increased with the raise in temperature in all “PEG-400 + water” mixtures studied. The highest and lowest solubility values of ECT were found in pure PEG-400 (1.45 × 10−1) at “T = 318.2 K” and pure water (7.95 × 10−3) at “T = 298.2 K”, respectively. The quantitative values of activity coefficients indicated higher interactions at molecular level in ECT and PEG-400 combination compared with ECT and water combination. “Apparent thermodynamic analysis” showed an “endothermic and entropy-driven dissolution” of ECT in all “PEG-400 + water” combinations studied. The solvation nature of ECT was found an “enthalpy-driven” in each “PEG-400 + water” mixture studied.

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“…TAF exhibited an improved antiviral activity and safety profile related to renal and bone toxicity [30][31][32]. Therefore, TFV, TDF and in particular TAF represent key compounds for the treatment of chronic hepatitis B and HIV infections and are thus a subject of intense research in the area of new drug delivery systems [33][34][35][36][37][38][39][40].…”

Section: Introductionmentioning

confidence: 99%

Co-crystals, Salts or Mixtures of Both? The Case of Tenofovir Alafenamide Fumarates

Lengauer

Makuc

Šterk³

et al. 2020

Pharmaceutics

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Tenofovir alafenamide fumarate (TAF) is the newest prodrug of tenofovir that constitutes several drug products used for the treatment of HIV/AIDS. Although the solid-state properties of its predecessor tenofovir disoproxil fumarate have been investigated and described in the literature, there are no data in the scientific literature on the solid state properties of TAF. In our report, we describe the preparation of two novel polymorphs II and III of tenofovir alafenamide monofumarate (TA MF2 and TA MF3). The solid-state structure of these compounds was investigated in parallel to the previously known tenofovir alafenamide monofumarate form I (TA MF1) and tenofovir alafenamide hemifumarate (TA HF). Interestingly, the single-crystal X-ray diffraction of TA HF revealed that this derivative exists as a co-crystal form. In addition, we prepared a crystalline tenofovir alafenamide free base (TA) and its hydrochloride salt (TA HCl), which enabled us to determine the structure of TA MF derivatives using 15N-ssNMR (15N-solid state nuclear magnetic resonance). Surprisingly, we observed that TA MF1 exists as a mixed ionization state complex or pure salt, while TA MF2 and TA MF3 can be obtained as pure co-crystal forms.

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Rational Development of Liposomal Hydrogels: A Strategy for Topical Vaginal Antiretroviral Drug Delivery in the Context of HIV Prevention

Cited by 41 publications

References 75 publications

Liposomal and Ethosomal Gels for the Topical Delivery of Anthralin: Preparation, Comparative Evaluation and Clinical Assessment in Psoriatic Patients

Liposomal and Ethosomal Gels for the Topical Delivery of Anthralin: Preparation, Comparative Evaluation and Clinical Assessment in Psoriatic Patients

Solubility, Hansen Solubility Parameters and Thermodynamic Behavior of Emtricitabine in Various (Polyethylene Glycol-400 + Water) Mixtures: Computational Modeling and Thermodynamics

Co-crystals, Salts or Mixtures of Both? The Case of Tenofovir Alafenamide Fumarates

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