QbD based approach for optimization of Tenofovir disoproxil fumarate loaded liquid crystal precursor with improved permeability

Patil, Sharvil; Kadam, Chandrashekhar; Pokharkar, Varsha

doi:10.1016/j.jare.2017.07.005

Cited by 20 publications

(10 citation statements)

References 39 publications

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“…In contrast, the three phospholipids, i.e., SPC, EPC, and HPMC, showed flat patterns, indicating their noncrystalline nature [ 35 , 36 ], whilst HSPC showed few peaks, indicating its liquid crystalline nature powder [ 37 ]. This liquid crystal nature is suitable for such bioavailability enhancement strategy of poorly permeable drugs [ 38 ].…”

Section: Resultsmentioning

confidence: 99%

Formulation Design and Cell Cytotoxicity of Curcumin-Loaded Liposomal Solid Gels for Anti-Hepatitis C Virus

Yusuf

Novitasari

Purnami

et al. 2022

Advances in Pharmacological and Pharmaceutical Sciences

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Backgrounds. Curcumin (CUR) is a low-molecular-weight polyphenolic substance obtained from the tuber part of Curcuma species. Anti-inflammatory and anti-hepatitis C virus (HCV) activities have been associated with CUR. However, its poor aqueous solubility and low systemic bioavailability have been the challenges in improving the therapeutic efficacy of curcumin. Aim. The study aimed to produce CUR-loaded liposomal solid gels as anti-HCV delivery systems. Parameters including the physical characteristics and the cell cytotoxicity properties were evaluated. Methods. The freeze-drying technique was applied to manufacture the CUR-loaded liposomal solid gels. Scanning electron microscopy (SEM), X-ray diffractometry (XRD), and differential thermal analysis (DTA) were involved to reveal the characteristics of the solid gels. Such characteristics were as follows: the morphology and the microscopic structure of the solid gels, the crystallinity structure of the curcumin, and the thermal properties of the mixtures. Furthermore, their cell cytotoxicity was investigated using a Huh7it cell line. Results. The SEM images confirmed that curcumin liposomes were intact and trapped in the solid gel matrix. The XRD data showed flat patterns diffractograms of the formulations, confirming the transformation of CUR from crystalline to amorphous form. The DTA thermograms showed a single melting endothermic peak at a higher temperature around 200°C, indicating a single-phase transition of the mixtures. The XRD and DTA data revealed the molecular dispersion of CUR in the developed formulations. The cytotoxicity data provided as cell cytotoxicity 50 (CC50) for all formulations were ≥25 mg. These data confirmed that the developed liposomal solid gels were not cytotoxic to Huh7it cell line, indicating that the anti-HCV activity would be through a specific pathway and not by its toxicity. Conclusion. The CUR-loaded liposomal solid gels exhibited the potential and offered an alternative dosage form to improve the therapeutic efficacy of curcumin as an anti-HCV.

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Section: Resultsmentioning

confidence: 99%

Formulation Design and Cell Cytotoxicity of Curcumin-Loaded Liposomal Solid Gels for Anti-Hepatitis C Virus

Yusuf

Novitasari

Purnami

et al. 2022

Advances in Pharmacological and Pharmaceutical Sciences

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“…SEM analysis could provide detailed surface images to investigate the structures and the morphology of intact TFR before and after β-CD:TFR inclusion complex formation. While TFR was seen as an irregular fiber-like crystal [45] , β-CD was seen as irregular crystalline particles of various sizes and shapes in the SEM image [44] . The original surface morphology of TFR and β-CD was lost, according to SEM analysis, in the β-CD:TFR inclusion complex, which appeared as particles with a smooth surface ( Fig.…”

Section: Resultsmentioning

confidence: 99%

Tenofovir antiviral drug solubility enhancement with β-cyclodextrin inclusion complex and in silico study of potential inhibitor against SARS-CoV-2 main protease (Mpro)

Mohandoss

Velu

Stalin

et al. 2023

Journal of Molecular Liquids

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“…TFV is notable for a band around 1700 cm −1 , corresponding to C=O stretching [27]. It also has bands at 3100 cm −1 and 3200 cm −1 corresponding to C–H and N–H bonds respectively [28] (Figure 1).…”

Section: Resultsmentioning

confidence: 99%

Tenofovir Hot-Melt Granulation using Gelucire® to Develop Sustained-Release Vaginal Systems for Weekly Protection against Sexual Transmission of HIV

et al. 2019

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Hot-melt granulation is a technique used to obtain granules by dispersing a drug in polymers at a high temperature. Tenofovir, an antiretroviral drug with proven activity as a vaginal microbicide, was dispersed in melted Gelucire® (or a mixture of different Gelucire®) to obtain drug-loaded granules. Studies performed on the granules proved that the drug is not altered in the hot-melt granulation process. The granules obtained were included in a matrix formed by the hydrophilic polymers hydroxypropylmethylcellulose and chitosan to obtain vaginal tablets that combine different mechanisms of controlled release: The Gelucire® needs to soften to allow the release of the Tenofovir, and the hydrophilic polymers must form a gel so the drug can diffuse through it. The studies performed with the tablets were swelling behavior, Tenofovir release, and ex vivo mucoadhesion. The tablets containing granules obtained with Tenofovir and Gelucire® 43/01 in a ratio of 1:2 in a matrix formed by hydroxypropylmethylcellulose and chitosan in a ratio of 1.9:1 were selected as the optimal formulation, since they release Tenofovir in a sustained manner over 216h and remain attached to the vaginal mucosa throughout. A weekly administration of these tablets would therefore offer women protection against the sexual transmission of HIV.

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QbD based approach for optimization of Tenofovir disoproxil fumarate loaded liquid crystal precursor with improved permeability

Abstract: Graphical abstract

Cited by 20 publications

References 39 publications

Formulation Design and Cell Cytotoxicity of Curcumin-Loaded Liposomal Solid Gels for Anti-Hepatitis C Virus

Formulation Design and Cell Cytotoxicity of Curcumin-Loaded Liposomal Solid Gels for Anti-Hepatitis C Virus

Tenofovir antiviral drug solubility enhancement with β-cyclodextrin inclusion complex and in silico study of potential inhibitor against SARS-CoV-2 main protease (Mpro)

Tenofovir Hot-Melt Granulation using Gelucire® to Develop Sustained-Release Vaginal Systems for Weekly Protection against Sexual Transmission of HIV

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