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  1. Article: Compritol-Based Nanostrucutured Lipid Carriers (NLCs) for Augmentation of Zolmitriptan Bioavailability via the Transdermal Route: In Vitro Optimization, Ex Vivo Permeation, In Vivo Pharmacokinetic Study.

    Hassan, Doaa H / Shohdy, Joseph N / El-Setouhy, Doaa Ahmed / El-Nabarawi, Mohamed / Naguib, Marianne J

    Pharmaceutics

    2022  Volume 14, Issue 7

    Abstract: Migraine is a severe neurovascular disease manifested mainly as unilateral throbbing headaches. Triptans are agonists for serotonin receptors. Zolmitriptan (ZMP) is a biopharmaceutics classification system (BCS) class III medication with an absolute oral ...

    Abstract Migraine is a severe neurovascular disease manifested mainly as unilateral throbbing headaches. Triptans are agonists for serotonin receptors. Zolmitriptan (ZMP) is a biopharmaceutics classification system (BCS) class III medication with an absolute oral bioavailability of less than 40%. As a result, our research intended to increase ZMP bioavailability by developing transdermal nanostructured lipid carriers (NLCs). NLCs were prepared utilizing a combination of hot melt emulsification and high-speed stirring in a 3
    Language English
    Publishing date 2022-07-18
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2527217-2
    ISSN 1999-4923
    ISSN 1999-4923
    DOI 10.3390/pharmaceutics14071484
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Statistical optimization of hyaluronic acid enriched ultradeformable elastosomes for ocular delivery of voriconazole via Box-Behnken design:

    Fahmy, Abdurrahman Muhammad / Hassan, Mariam / El-Setouhy, Doaa Ahmed / Tayel, Saadia Ahmed / Al-Mahallawi, Abdulaziz Mohsen

    Drug delivery

    2020  Volume 28, Issue 1, Page(s) 77–86

    Abstract: Voriconazole (VCZ) is a well-known broad spectrum triazole antifungal, mainly used orally and intravenously. The study aimed to formulate VCZ into ultradeformable elastosomes for the topical treatment of ocular fungal keratitis. Different formulae were ... ...

    Abstract Voriconazole (VCZ) is a well-known broad spectrum triazole antifungal, mainly used orally and intravenously. The study aimed to formulate VCZ into ultradeformable elastosomes for the topical treatment of ocular fungal keratitis. Different formulae were prepared using a modified ethanol injection method, employing a 3
    MeSH term(s) Administration, Topical ; Animals ; Antifungal Agents/administration & dosage ; Candida albicans/drug effects ; Chemistry, Pharmaceutical ; Drug Carriers/chemistry ; Humans ; Hyaluronic Acid/chemistry ; Male ; Particle Size ; Rabbits ; Surface Properties ; Voriconazole/administration & dosage
    Chemical Substances Antifungal Agents ; Drug Carriers ; Hyaluronic Acid (9004-61-9) ; Voriconazole (JFU09I87TR)
    Language English
    Publishing date 2020-12-19
    Publishing country England
    Document type Journal Article
    ZDB-ID 1213261-5
    ISSN 1521-0464 ; 1071-7544
    ISSN (online) 1521-0464
    ISSN 1071-7544
    DOI 10.1080/10717544.2020.1858997
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Voriconazole Ternary Micellar Systems for the Treatment of Ocular Mycosis: Statistical Optimization and In Vivo Evaluation.

    Fahmy, Abdurrahman Muhammad / Hassan, Mariam / El-Setouhy, Doaa Ahmed / Tayel, Saadia Ahmed / Al-Mahallawi, Abdulaziz Mohsen

    Journal of pharmaceutical sciences

    2020  Volume 110, Issue 5, Page(s) 2130–2138

    Abstract: Voriconazole (VRC) is a broad spectrum, second generation triazole antifungal. The main use of VRC is via the oral and intravenous route. The study aimed to formulate VRC into ternary micellar systems (TMSs) for the topical treatment of ocular mycosis. ... ...

    Abstract Voriconazole (VRC) is a broad spectrum, second generation triazole antifungal. The main use of VRC is via the oral and intravenous route. The study aimed to formulate VRC into ternary micellar systems (TMSs) for the topical treatment of ocular mycosis. TMSs were successfully prepared by water addition/solvent evaporation method, applying a 3-factor D-optimal design. The numerical optimization process suggested an optimal formula (OTMS) composed of total Pluronics to drug weight ratio of 22.89: 1, 1:1 weight ratio of Pluronic® P123 and F68, and 2% w/v of Labrasol. OTMS had high solubilization efficiency of 98.0%, small micellar size of 21.8 nm and suitable zeta potential and polydispersity index values of -9.0 mV and 0.261, respectively. OTMS exhibited acceptable stability for 3 months. Transmission electron microscopy demonstrated the spherical morphology of micelles. OTMS was expected to cause no ocular irritation or blurring in vision as reflected by pH and refractive index measurements. The histopathological study revealed the safety of OTMS for ocular use. The fungal susceptibility testing using Candida albicans demonstrated the superiority of OTMS to VRC suspension, with greater and more durable growth inhibition. Therefore, ocular application of optimized VRC-loaded TMSs can be a promising treatment for ocular mycosis.
    MeSH term(s) Antifungal Agents/therapeutic use ; Drug Carriers/therapeutic use ; Drug Delivery Systems ; Eye Infections, Fungal/drug therapy ; Humans ; Micelles ; Particle Size ; Voriconazole/therapeutic use
    Chemical Substances Antifungal Agents ; Drug Carriers ; Micelles ; Voriconazole (JFU09I87TR)
    Language English
    Publishing date 2020-12-17
    Publishing country United States
    Document type Journal Article
    ZDB-ID 3151-3
    ISSN 1520-6017 ; 0022-3549
    ISSN (online) 1520-6017
    ISSN 0022-3549
    DOI 10.1016/j.xphs.2020.12.013
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Enhancement of Transdermal Delivery of Haloperidol via Spanlastic Dispersions: Entrapment Efficiency vs. Particle Size.

    Fahmy, Abdurrahman M / El-Setouhy, Doaa Ahmed / Habib, Basant A / Tayel, Saadia A

    AAPS PharmSciTech

    2019  Volume 20, Issue 3, Page(s) 95

    Abstract: Haloperidol (Hal) is a well-known typical antipsychotic. Hepatic first pass metabolism leads to its limited oral bioavailability. This study aimed at enhancing transdermal delivery of Hal via spanlastic formulae. Hal-loaded spanlastics of Span®60 and an ... ...

    Abstract Haloperidol (Hal) is a well-known typical antipsychotic. Hepatic first pass metabolism leads to its limited oral bioavailability. This study aimed at enhancing transdermal delivery of Hal via spanlastic formulae. Hal-loaded spanlastics of Span®60 and an edge activator (EA) were successfully prepared by ethanol injection method according to a 3
    MeSH term(s) Administration, Cutaneous ; Animals ; Animals, Newborn ; Antipsychotic Agents/administration & dosage ; Antipsychotic Agents/chemistry ; Antipsychotic Agents/pharmacokinetics ; Biological Availability ; Drug Carriers/metabolism ; Drug Compounding ; Haloperidol/administration & dosage ; Haloperidol/chemistry ; Haloperidol/pharmacokinetics ; Particle Size ; Polysorbates ; Rats ; Skin/metabolism ; Skin Absorption
    Chemical Substances Antipsychotic Agents ; Drug Carriers ; Polysorbates ; Haloperidol (J6292F8L3D)
    Language English
    Publishing date 2019-01-29
    Publishing country United States
    Document type Journal Article
    ISSN 1530-9932
    ISSN (online) 1530-9932
    DOI 10.1208/s12249-019-1306-2
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Particle engineering/different film approaches for earlier absorption of meloxicam.

    Farid, Motaz / El-Setouhy, Doaa Ahmed / El-Nabarawi, Mohamed Ahmed / El-Bayomi, Tahany

    Drug delivery

    2016  Volume 23, Issue 7, Page(s) 2309–2317

    Abstract: Meloxicam (Mel) is a non-steroidal potent anti-inflammatory drug with effective analgesic effect for various situations; e.g. postoperative pain. The early systemic exposure to Mel and hence the rapid onset of pharmacological action is limited by its ... ...

    Abstract Meloxicam (Mel) is a non-steroidal potent anti-inflammatory drug with effective analgesic effect for various situations; e.g. postoperative pain. The early systemic exposure to Mel and hence the rapid onset of pharmacological action is limited by its poor water solubility; a situation which may be more pronounced during acute pain episode because of reduced gastric motility that affects disintegration and dissolution of solid dosage forms. To overcome delayed absorption of Mel, improvement in the dissolution behavior of Mel is essential. Firstly, Mel spherical crystalline agglomerates (SCA) were prepared. Secondly, selected Mel SCA were integrated into intraoral fast disintegrating (OF) and edible (EF) films, they possess larger surface area that leads to rapid disintegration and release of the drug into the oral cavity within seconds and hence a rapid onset of action could be achieved. Stability study of formulations resulting in faster and higher extent of dissolution and suitable mechanical properties (G3 and G12) revealed their physical and chemical stability after three months of storage under different conditions. Both G3 and G12 successfully offered rapid absorption rate and accordingly an earlier systemic exposure to Mel compared to Mobic tablets as revealed by significantly earlier T
    MeSH term(s) Administration, Oral ; Anti-Inflammatory Agents, Non-Steroidal/administration & dosage ; Anti-Inflammatory Agents, Non-Steroidal/chemistry ; Anti-Inflammatory Agents, Non-Steroidal/pharmacology ; Humans ; Particle Size ; Solubility ; Thiazines/administration & dosage ; Thiazines/chemistry ; Thiazines/pharmacology ; Thiazoles/administration & dosage ; Thiazoles/chemistry ; Thiazoles/pharmacology
    Chemical Substances Anti-Inflammatory Agents, Non-Steroidal ; Thiazines ; Thiazoles ; meloxicam (VG2QF83CGL)
    Language English
    Publishing date 2016-09
    Publishing country England
    Document type Journal Article
    ZDB-ID 1213261-5
    ISSN 1521-0464 ; 1071-7544
    ISSN (online) 1521-0464
    ISSN 1071-7544
    DOI 10.3109/10717544.2014.982262
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: Bioenhanced sublingual tablet of drug with limited permeability using novel surfactant binder and microencapsulated polysorbate: In vitro/in vivo evaluation.

    El-Setouhy, Doaa Ahmed / Basalious, Emad B / Abdelmalak, Nevine Shawky

    European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V

    2015  Volume 94, Page(s) 386–392

    Abstract: Formulation of sublingual tablets of drugs with limited permeability poses a great challenge due to their poor absorption. In this study, bioenhanced sublingual tablets (BESTs) of zolmitriptan were prepared using novel surfactant binder (Pluronic® p123/ ... ...

    Abstract Formulation of sublingual tablets of drugs with limited permeability poses a great challenge due to their poor absorption. In this study, bioenhanced sublingual tablets (BESTs) of zolmitriptan were prepared using novel surfactant binder (Pluronic® p123/Syloid® mixture) to enhance tablet disintegration and dissolution. Microencapsulated polysorbate 80 (Sepitrap™ 80) were included in the composition of BESTs to enhance the drug transport through the sublingual mucosa. Tablets were evaluated for in vitro/in vivo disintegration, in vitro dissolution and ex vivo permeation. Solubility studies confirmed that phosphate buffer; pH 6.8 could be used as dissolution medium for sublingual tablets of zolmitriptan. BEST-5 containing Pluronic® p123/Syloid® mixture and Sepitrap™ 80 exhibited the shortest in vitro/in vivo disintegration times (<30s), the highest dissolution at early time dissolution points and the highest enhancement of drug transport through mucosal membrane. The in vivo pharmacokinetic study using human volunteers showed a significant increase in the rate and extent of sublingual absorption with less variations of Tmax after sublingual administration of both BEST-5 and Zomig-ZMT ODT. Our results proposed that Pluronic® p123/Syloid® mixture and Sepitrap™ 80 could be promising for the development of sublingual tablets for rapid onset of action of drugs with limited permeability.
    MeSH term(s) Administration, Sublingual ; Animals ; Area Under Curve ; Chickens ; Drug Compounding ; Excipients/chemistry ; Healthy Volunteers ; Humans ; Oral Mucosal Absorption ; Oxazolidinones/administration & dosage ; Oxazolidinones/chemistry ; Oxazolidinones/pharmacokinetics ; Permeability ; Poloxalene/chemistry ; Polysorbates/chemistry ; Silicon Dioxide/chemistry ; Solubility ; Surface-Active Agents/chemistry ; Tablets ; Tissue Distribution ; Tryptamines/administration & dosage ; Tryptamines/chemistry ; Tryptamines/pharmacokinetics
    Chemical Substances Excipients ; Oxazolidinones ; Polysorbates ; Surface-Active Agents ; Tablets ; Tryptamines ; pluronic block copolymer P123 (2E9U4Y94DB) ; zolmitriptan (2FS66TH3YW) ; Silicon Dioxide (7631-86-9) ; Poloxalene (9003-11-6)
    Language English
    Publishing date 2015-06-15
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 1065368-5
    ISSN 1873-3441 ; 0939-6411
    ISSN (online) 1873-3441
    ISSN 0939-6411
    DOI 10.1016/j.ejpb.2015.06.006
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  7. Article ; Online: Intranasal haloperidol-loaded miniemulsions for brain targeting: Evaluation of locomotor suppression and in-vivo biodistribution.

    El-Setouhy, Doaa Ahmed / Ibrahim, A B / Amin, Maha M / Khowessah, Omneya M / Elzanfaly, Eman S

    European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences

    2016  Volume 92, Page(s) 244–254

    Abstract: Haloperidol is a commonly prescribed antipsychotic drug currently administered as oral and injectable preparations. This study aimed to prepare haloperidol intranasal miniemulsion helpful for psychiatric emergencies and exhibiting lower systemic exposure ...

    Abstract Haloperidol is a commonly prescribed antipsychotic drug currently administered as oral and injectable preparations. This study aimed to prepare haloperidol intranasal miniemulsion helpful for psychiatric emergencies and exhibiting lower systemic exposure and side effects associated with non-target site delivery. Haloperidol miniemulsions were successfully prepared by spontaneous emulsification adopting 2(3) factorial design. The effect of three independent variables at two levels each namely; oil type (Capmul®-Capryol™90), lipophilic emulsifier type (Span 20-Span 80) and HLB value (12-14) on globule size, PDI and percent locomotor activity inhibition in mice was evaluated. The optimized formula (F4, Capmul®, Tween 80/Span 20, HLB 14) showed globule size of 209.5±0.98nm, PDI of 0.402±0.03 and locomotor inhibition of 83.89±9.15% with desirability of 0.907. Biodistribution study following intranasal and intravenous administration of the radiolabeled (99m)Tc mucoadhesive F4 revealed that intranasal administration achieved 1.72-fold higher and 6 times faster peak brain levels compared with intravenous administration. Drug targeting efficiency percent and brain/blood exposure ratios remained above 100% and 1 respectively after intranasal instillation compared to a maximum brain/blood exposure ratio of 0.8 post intravenous route. Results suggested the CNS delivery of major fraction of haloperidol via direct transnasal to brain pathway that can be a promising alternative to oral and parenteral routes in chronic and acute situations. Haloperidol concentration of 275.6ng/g brain 8h post intranasal instillation, higher than therapeutic concentration range of haloperidol (0.8 to 5.15ng/ml), suggests possible sustained delivery of the drug through nasal route.
    MeSH term(s) Adhesiveness ; Administration, Intranasal ; Animals ; Antipsychotic Agents/administration & dosage ; Antipsychotic Agents/chemistry ; Antipsychotic Agents/pharmacokinetics ; Antipsychotic Agents/pharmacology ; Brain/metabolism ; Drug Delivery Systems ; Drug Stability ; Emulsions ; Haloperidol/administration & dosage ; Haloperidol/chemistry ; Haloperidol/pharmacokinetics ; Haloperidol/pharmacology ; Locomotion ; Mice ; Nasal Mucosa/chemistry ; Rabbits ; Solubility ; Tissue Distribution
    Chemical Substances Antipsychotic Agents ; Emulsions ; Haloperidol (J6292F8L3D)
    Language English
    Publishing date 2016-09-20
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 1154366-8
    ISSN 1879-0720 ; 0928-0987
    ISSN (online) 1879-0720
    ISSN 0928-0987
    DOI 10.1016/j.ejps.2016.05.002
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article ; Online: Provesicular granisetron hydrochloride buccal formulations: in vitro evaluation and preliminary investigation of in vivo performance.

    Ahmed, Sami / El-Setouhy, Doaa Ahmed / El-Latif Badawi, Alia Abd / El-Nabarawi, Mohamed Ahmed

    European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences

    2014  Volume 60, Page(s) 10–23

    Abstract: Granisetron hydrochloride (granisetron) is a potent antiemetic that has been proven to be effective in acute and delayed emesis in cancer chemotherapy. Granisetron suffers from reduced oral bioavailability (≈60%) due to hepatic metabolism. In this study ... ...

    Abstract Granisetron hydrochloride (granisetron) is a potent antiemetic that has been proven to be effective in acute and delayed emesis in cancer chemotherapy. Granisetron suffers from reduced oral bioavailability (≈60%) due to hepatic metabolism. In this study the combined advantage of provesicular carriers and buccal drug delivery has been explored aiming to sustain effect and improve bioavailability of granisetron via development of granisetron provesicular buccoadhesive tablets with suitable quality characteristics (hardness, drug content, in vitro release pattern, exvivo bioadhesion and in vivo bioadhesion behavior). Composition of the reconstituted niosomes from different prepared provesicular carriers regarding type of surfactant used and cholesterol concentration significantly affected both entrapment efficiency (%EE) and vesicle size. Span 80 proniosome-derived niosomes exhibited higher encapsulation efficiency and smaller particle size than those derived from span 20. Also, the effect of %EE and bioadhesive polymer type on in vitro drug release and in vivo performance of buccoadhesive tablets was investigated. Based on achievement of required in vitro release pattern (20-30% at 2h, 40-65% at 6h and 80-95% at 12h), in vivo swelling behavior, and in vivo adhesion time (>14 h) granisetron formulation (F19, 1.4 mg) comprising HPMC:carbopol 974P (7:3) and maltodextrin coated with the vesicular precursors span 80 and cholesterol (9:1) was chosen for in vivo study. In vivo pharmacokinetic study revealed higher bioavailability of buccal formulation relative to conventional oral formulation of granisetron (AUC0-∞ is 89.97 and 38.18 ng h/ml for buccal and oral formulation, respectively). A significantly lower and delayed Cmax (12.09±4.47 ng/ml, at 8h) was observed after buccal application compared to conventional oral tablet (31.66±10.15 ng/ml, at 0.5 h). The prepared provesicular buccoadhesive tablet of granisetron (F19) might help bypass hepatic first-pass metabolism and improve bioavailability of granisetron with the possibility of reducing reported daily dose (2mg) and reducing dosing frequency.
    MeSH term(s) Adhesiveness ; Administration, Buccal ; Adult ; Animals ; Antiemetics/administration & dosage ; Antiemetics/blood ; Antiemetics/chemistry ; Antiemetics/pharmacokinetics ; Biological Availability ; Chemistry, Pharmaceutical ; Chickens ; Cholesterol/chemistry ; Granisetron/administration & dosage ; Granisetron/blood ; Granisetron/chemistry ; Granisetron/pharmacokinetics ; Hardness ; Hexoses/chemistry ; Humans ; In Vitro Techniques ; Male ; Mouth Mucosa/chemistry ; Mouth Mucosa/metabolism ; Polysaccharides/chemistry ; Rabbits ; Tablets
    Chemical Substances Antiemetics ; Hexoses ; Polysaccharides ; Tablets ; sorbitan monooleate (06XEA2VD56) ; sorbitan monolaurate (6W9PS8B71J) ; maltodextrin (7CVR7L4A2D) ; Cholesterol (97C5T2UQ7J) ; Granisetron (WZG3J2MCOL)
    Language English
    Publishing date 2014-08-18
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 1154366-8
    ISSN 1879-0720 ; 0928-0987
    ISSN (online) 1879-0720
    ISSN 0928-0987
    DOI 10.1016/j.ejps.2014.04.013
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  9. Article ; Online: Comparative study on the in vitro performance of blister molded and conventional lornoxicam immediate release liquitablets: accelerated stability study and anti-inflammatory and ulcerogenic effects.

    El-Setouhy, Doaa Ahmed / Gamiel, Alaa Abdel-Rahman / Badawi, Alia Abd El-Latif / Osman, Afaf Sayed / Labib, Dina Ahmed

    Pharmaceutical development and technology

    2017  Volume 22, Issue 2, Page(s) 256–265

    Abstract: Context: Lornoxicam is a potent non-steroidal anti-inflammatory drug (NSAID). It shows limited solubility in the gastric pH, delayed bioavailability and pharmacodynamic effects with aggravated gastric side effects (due to longer residence in the stomach ...

    Abstract Context: Lornoxicam is a potent non-steroidal anti-inflammatory drug (NSAID). It shows limited solubility in the gastric pH, delayed bioavailability and pharmacodynamic effects with aggravated gastric side effects (due to longer residence in the stomach wall).
    Objective: To enhance dissolution of lornoxicam in the gastric fluid and expectedly absorption and pharmacological action, with less ulcerogenic effects.
    Materials and methods: Formulation of immediate release (IR) lornoxicam liquitablets containing both liquid and solid release modulators (wetting agent, solubilizers and microenvironmental pH modifiers). Beside the traditional direct compression technique employed for the preparation of liquitablets a new technique, blister molding, was also used. The effect of the two different manufacturing methods on the fast release characteristics (rapid disintegration and dissolution) was studied. Stability and pharmacological activity of the optimum formula were also explored.
    Results: Similarity factor pointed out the superiority of molding technique in enhancing dissolution of lornoxicam owing to significant crystallinity reduction (XRD). Optimum formula showed negligible change in drug content and dissolution profiles over 12 weeks, significantly improved anti-inflammatory activity and significantly reduced gastric ulcerative effect over pure lornoxicam and commercial formula.
    Discussion and conclusion: Blister molded lornoxicam liquitablet of improved dissolution and pharmacological activity and less gastric erosion was successfully prepared.
    MeSH term(s) Animals ; Anti-Inflammatory Agents, Non-Steroidal/administration & dosage ; Anti-Inflammatory Agents, Non-Steroidal/adverse effects ; Anti-Inflammatory Agents, Non-Steroidal/chemistry ; Anti-Inflammatory Agents, Non-Steroidal/therapeutic use ; Arthritis/drug therapy ; Delayed-Action Preparations/chemistry ; Drug Compounding ; Drug Liberation ; Drug Stability ; Piroxicam/administration & dosage ; Piroxicam/adverse effects ; Piroxicam/analogs & derivatives ; Piroxicam/chemistry ; Piroxicam/therapeutic use ; Rats ; Solubility ; Tablets ; Ulcer/chemically induced
    Chemical Substances Anti-Inflammatory Agents, Non-Steroidal ; Delayed-Action Preparations ; Tablets ; Piroxicam (13T4O6VMAM) ; lornoxicam (ER09126G7A)
    Language English
    Publishing date 2017-03
    Publishing country England
    Document type Comparative Study ; Journal Article
    ZDB-ID 1331774-x
    ISSN 1097-9867 ; 1083-7450
    ISSN (online) 1097-9867
    ISSN 1083-7450
    DOI 10.1080/10837450.2016.1221423
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  10. Article ; Online: Penetration enhancer-containing spanlastics (PECSs) for transdermal delivery of haloperidol: in vitro characterization, ex vivo permeation and in vivo biodistribution studies.

    Fahmy, Abdurrahman M / El-Setouhy, Doaa Ahmed / Ibrahim, Ahmed B / Habib, Basant A / Tayel, Saadia A / Bayoumi, Noha A

    Drug delivery

    2017  Volume 25, Issue 1, Page(s) 12–22

    Abstract: Haloperidol (Hal) is one of the widely used antipsychotic drugs. When orally administered, it suffers from low bioavailability due to hepatic first pass metabolism. This study aimed at developing Hal-loaded penetration enhancer-containing spanlastics ( ... ...

    Abstract Haloperidol (Hal) is one of the widely used antipsychotic drugs. When orally administered, it suffers from low bioavailability due to hepatic first pass metabolism. This study aimed at developing Hal-loaded penetration enhancer-containing spanlastics (PECSs) to increase transdermal permeation of Hal with sustained release. PECSs were successfully prepared using ethanol injection method showing reasonable values of percentage entrapment efficiency, particle size, polydispersity index and zeta potential. The statistical analysis of the ex vivo permeation parameters led to the choice of F1L - made of Span
    MeSH term(s) Administration, Cutaneous ; Animals ; Antipsychotic Agents/administration & dosage ; Antipsychotic Agents/chemistry ; Biological Availability ; Chemistry, Pharmaceutical/methods ; Delayed-Action Preparations/administration & dosage ; Delayed-Action Preparations/chemistry ; Drug Carriers/chemistry ; Drug Delivery Systems/methods ; Haloperidol/administration & dosage ; Haloperidol/chemistry ; Hydrogel, Polyethylene Glycol Dimethacrylate/administration & dosage ; Hydrogel, Polyethylene Glycol Dimethacrylate/chemistry ; Hydrogen-Ion Concentration ; Mice ; Particle Size ; Permeability/drug effects ; Rats ; Skin/metabolism ; Skin Absorption/drug effects ; Tissue Distribution/drug effects
    Chemical Substances Antipsychotic Agents ; Delayed-Action Preparations ; Drug Carriers ; Hydrogel, Polyethylene Glycol Dimethacrylate (25852-47-5) ; Haloperidol (J6292F8L3D)
    Language English
    Publishing date 2017-12-06
    Publishing country England
    Document type Journal Article
    ZDB-ID 1213261-5
    ISSN 1521-0464 ; 1071-7544
    ISSN (online) 1521-0464
    ISSN 1071-7544
    DOI 10.1080/10717544.2017.1410262
    Database MEDical Literature Analysis and Retrieval System OnLINE

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