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Mehreen Bashir,1 Junaid Ahmad,1 Muhammad Asif,2 Salah-Ud-Din Khan,3 Muhammad Irfan,1 Asim Y Ibrahim,4 Sajid Asghar,1 Ikram Ullah Khan,1 Muhammad Shahid Iqbal,5 Abdul Haseeb,6 Syed Haroon Khalid,1 Mohammed AS Abourehab7,8 1Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University, Faisalabad, 38000, Pakistan; 2Department of Pharmacology, Faculty of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, Pakistan; 3Department of Biochemistry, College of Medicine, Imam Mohammad Ibn Saud Islamic University, Riyadh, Saudi Arabia; 4Faculty of Pharmacy, Omdurman Islamic University, Omdurman, Sudan; 5Department of Clinical Pharmacy, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj, Saudi Arabia; 6Department of Clinical Pharmacy, College of Pharmacy, Umm Al-Qura University, Makkah, 21955, Saudi Arabia; 7Department of Pharmaceutics, Faculty of Pharmacy, Umm Al-Qura University, Makkah, Saudi Arabia; 8Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia, EgyptCorrespondence: Syed Haroon KhalidDepartment of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University, Faisalabad, 38000, PakistanTel +92-3166752223Email syedharoonkhalid@gcuf.edu.pkPurpose: Rheumatoid arthritis is an autoimmune disorder that directly affects joints. However, other body organs including heart, eyes, skin, blood vessels and lungs may also be affected. The purpose of this study was to design and evaluate a nanoemulgel formulation of diflunisal (DIF) and solubility enhanced diflunisal (DIF-IC) for enhanced topical anti-inflammatory activity.Methodology: Nanoemulsion formulations of both DIF and DIF-IC were prepared and incorporated in three different gelling agents, namely carboxymethylcellulose sodium (CMC-Na), sodium alginate (Na-ALG) and xanthan gum (XG). All the formulations were evaluated in term of particle size, pH, conductivity, viscosity, zeta potential and in vitro drug release. The formulation 2 (NE2) of both DIF and DIF-IC which expressed optimum release and satisfactory physicochemical properties was incorporated with gelling agents to produce final nanoemulgel formulations. The optimized nanoemulgel formulation was subjected to three different in vivo anti-inflammatory models including carrageenan-induced paw edema model, histamine-induced paw edema model and formalin-induced paw edema model.Results: DIF-IC-loaded nanoemulgel formulations yielded significantly enhanced in vitro skin permeation than DIF-loaded nanoemulgel. The nanoemulgel formulation of DIF-IC formulated with XG produced improved in vivo anti-inflammatory activity.Conclusion: It was recommended that DIF-IC-based nanoemulgel formulation prepared with XG could be a better option for effective topical treatment of inflammatory conditions.Keywords: diflunisal, nanoemulsion, pseudoternary phase diagram, in vitro skin permeation, anti-inflammatory activity, improved efficacy

Malik Muhammad Irfan,1,2 Shefaat Ullah Shah,1,2 Ikram Ullah Khan,3 Muhammad Usman Munir,4 Nauman Rahim Khan,1,2 Kifayat Ullah Shah,1 Saif Ur Rehman,5 Muhammad Sohaib,1,2 Hafiz Muhammad Basit,1,2 Saima Mahmood1,2 1Department of Pharmaceutics, Faculty of Pharmacy, Gomal University, D.I. Khan, 29050, KPK, Pakistan; 2Gomal Centre for Skin/Regenerative Medicine and Drug Delivery Research (GCSRDDR), Faculty of Pharmacy, Gomal University, D.I. Khan, 29050, KPK, Pakistan; 3Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University, Faisalabad, Pakistan; 4Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University Sakaka, Aljouf, 72388, Saudi Arabia; 5Department of Pharmacy, Faculty of Medical and Health Sciences, University of Poonch, Rawlakot, AJK, PakistanCorrespondence: Shefaat Ullah ShahDepartment of Pharmaceutics, Faculty of Pharmacy, Gomal University, D.I. Khan, PakistanTel +92-336-514 0 682Email shefaatbu@gmail.comIntroduction: The current work aimed to formulate a novel chitosan-based finasteride nanosystem (FNS-NS) for skin delivery to optimize the drug availability in skin for a longer time and enhance ex vivo performance of finasteride against androgenic alopecia.Methods: Both undecorated and chitosan decorated FNS-NSs were synthesized by a high energy emulsification technique. All the prepared nanosystems were further subjected to physicochemical characterizations like pH, viscosity, encapsulation efficiency, surface morphology and in vitro drug release behavior. The influence of the nanosystem on the drug permeation and retention in rat skin was examined using Franz diffusion cell apparatus.Results: The droplet size of developed nanosystems ranged from 41 to 864 nm with a low polydispersity index. The zeta potential of the nanosystems was between -10 mV and +56 mV. This chitosan decorated nanosystem exhibited controlled drug release, ie about 78– 97% in 24 h. Among all the nanosystems, our chitosan decorated formulation (F5) had low drug permeation (16.35 μg/cm2) and higher drug retention (10.81 μg/cm2).Conclusion: The abovementioned results demonstrate satisfactory in vitro drug release, skin retention profiles and ex vivo performance with chitosan decorated FNS-NS (F5). This optimized formulation could increase drug availability in skin and could become a promising carrier for topical delivery to treat androgenic alopecia.Keywords: finasteride, nanosystem, solubility, chitosan, permeation, retention, androgenic alopecia

Lin Zhao, 1 Omer Mustapha, 2 Shumaila Shafique, 2 Talha Jamshaid, 3 Fakhar ud Din, 4 Yasir Mehmood, 5 Khaleeq Anwer, 6 Qurrat ul Ain Yousafi, 7 Talib Hussain, 8 Ikram Ullah Khan, 5 Muhammad Usman Ghori, 9 Yasser Shahzad, 8 Abid Mehmood Yousaf 8 1Department of Rheumatology of Traditional Chinese and Western Medicine, Xinxiang Central Hospital, Xinxiang 453000, People’s Republic of China; 2Faculty of Pharmaceutical Sciences, Dow College of Pharmacy, Dow University of Health Sciences, Karachi 74200, Pakistan; 3Faculty of Pharmacy and Alternative Medicine, Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan; 4Department of Pharmacy, Quaid-i-Azam University, Islamabad 45320, Pakistan; 5Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad 38040, Pakistan; 6Office of Chief Executive Officer, District Health Authority, Pakpattan 57400, Pakistan; 7Department of Neurosurgery, District Headquarters Hospital, Rawalpindi 46000, Pakistan; 8Department of Pharmacy, COMSATS University Islamabad, Lahore Campus, Lahore 54000, Pakistan; 9Department of Pharmacy, School of Applied Science, University of Huddersfield, Huddersfield HD1 3DH, UKCorrespondence: Abid Mehmood Yousaf Tel +92-300-477-4147; +92-345-722-0536Email abid.ucp@hotmail.com Email talib.hussain@cuilahore.edu.pkBackground: Piroxicam exhibits low oral bioavailability, due to its meager solubility in water. The intent of this study was to ameliorate the bioavailability of the drug by employing a solubility-enhancing encapsulation technique.Methods: Seven samples were formulated with piroxicam and gelatin using both solvent evaporation and electrospraying together. Evaluation of solubility and release rate in water and assessment of bioavailability in rats were carried out in comparison with piroxicam plain drug powder (PPDP). Other in vitro explorations were accomplished using powder X-ray diffraction analysis, differential scanning calorimetry, thermogravimetric analysis, scanning electron microscopy, and Fourier-transform infrared spectroscopy.Results: All piroxicam-loaded gelatinnanocontainers (PLGNs) enhanced solubility and release of the payload in water. In particular, a PLGN formulation consisting of piroxicam and gelatin at a 1:8 (w:w) ratio presented about 600-fold the drug solubility of that shown by PPDP. Moreover, 85.12%± 10.96% of the payload was released from this formulation in 10 minutes which was significantly higher than that dissolved from PPDP in 10 minutes (11.81%± 5.34%). Drug content, drug loading, and encapsulation efficiency of this formulation were 93.41%± 0.56%, 10.45%± 0.06%, and 66.74%± 6.87%, respectively. The drug loaded in PLGNs existed in the amorphous state, as confirmed by X-ray diffraction and differential scanning–calorimetry analyses, and was more stable when analyzed by thermogravimetric analysis. Moreover, Fourier-transform infrared spectroscopy analysis suggested nonexistence of any piroxicam–gelatin interaction in the formulation. In the scanning electron–microscopy image, PLGNs appeared as round, smooth particles, with particle size of < 1,000 nm. Amelioration in bioavailability of piroxicam with the aforementioned PLGN formulation was fourfold that of PPDP.Conclusion: The PLGN formulation fabricated with piroxicam and gelatin at 1:8 (w:w) might be a promising system for enhanced biopharmaceutical performance of the drug.Keywords: aqueous solubility, electrospraying, gelatin encapsulation, nanocontainers, oral bioavailability, piroxicam

Ru Sun, 1 Chengwu Shen, 1 Shumaila Shafique, 2 Omer Mustapha, 2 Talib Hussain, 3 Ikram Ullah Khan, 4 Yasir Mehmood, 4 Khaleeq Anwer, 5 Yasser Shahzad, 3 Abid Mehmood Yousaf 3 1Department of Pharmacy, Shandong Provincial Hospital, Shandong University, Jinan, Shandong 250000, People’s Republic of China; 2Faculty of Pharmaceutical Sciences, Dow College of Pharmacy, Dow University of Health Sciences, Karachi 74200, Pakistan; 3Department of Pharmacy, COMSATS University Islamabad, Lahore 54000, Pakistan; 4Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad 38000, Pakistan; 5Office of Chief Executive Officer, District Health Authority, Pakpattan 57400, PakistanCorrespondence: Abid Mehmood Yousaf; Talib HussainDepartment of Pharmacy, COMSATS University Islamabad, Lahore Campus, Lahore 54000, PakistanTel +92-300-4774147; +92-345-7220536Email abid.ucp@hotmail.com; talib.hussain@cuilahore.edu.pkBackground: Bezafibrate is a BCS class II drug as it presents very low solubility in water; therefore, its bioavailability after oral administration is very poor. The aim of this work was to enhance solubility and dissolution rate of bezafibrate in water in order to enhance its oral bioavailability.Methods: Several formulations were prepared using PVP K30 and Cremophor ELP employing the solvent-evaporation method and the electrospraying technique. Solubility, release rate, bioavailability in male Sprague Dawley rats, and lipid profile attributes in Wistar rats were assessed in comparison with bezafibrate plain powder. Solid-state characterization was carried out using X-ray diffraction (XRD) analysis, differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) spectroscopy and scanning electron microscopy (SEM).Results: All the formulations exerted positive effect towards the desired goal. In particular, the optimized formulation furnished about 14-fold enhanced solubility and 85.48 ± 10.16% drug was released in 10 min as compared with bezafibrate alone (4.06 ± 2.59%). The drug existed in the amorphous state in the prepared sample as confirmed by XRD and DSC, whilst no drug-excipient interactions were observed through FTIR analysis. Moreover, SEM revealed smooth-surfaced spherical particles of the optimized formulation. A 5.5-fold higher oral bioavailability was achieved with the optimized formulation in comparison with bezafibrate plain powder. Also, TG, LDL and TC were decreased, and HDL was increased considerably in HFD-treated rats.Conclusion: The optimized formulation consisting of bezafibrate, PVP K30 and cremophor ELP (1/12/1.5, w/w/w) might be a capable drug delivery system for orally administering poorly water-soluble bezafibrate with improved bioavailability and antihyperlipidemic effects.Keywords: aqueous solubility, bezafibrate, electrospraying, lipid profile, oral bioavailability, solid dispersion