Oral transmucosal drug delivery Mohammed Sattar, Majella E. Lane Drug Delivery Approaches Perspectives from Pharmacokinetics and Pharmacodynamics, 2021
Use of buccal morphine in the management of pain in children with life-limiting conditions: Results of a laboratory study Renée McCulloch, Mohammed Sattar, Ellen M Henderson, Majella E Lane, Myra Bluebond-Langner Palliative Medicine, 2018 Background: Children and infants with impaired swallow or compromised enteral absorption require alternative routes for administration of analgesia. Recent clinical guidance and practice for paediatric palliative care teams, who often treat such children, supports buccal morphine sulphate as a fast acting, effective and easily administered agent for pain relief. However, a consideration of the physicochemical properties and potency of morphine would suggest that it is not a suitable candidate for delivery via the transmucosal route, raising questions about its use in children and infants. Aim: To explore the permeability of buccal morphine sulphate in an established ex vivo porcine buccal mucosa as a necessary step in examining efficacy for use in children with life-limiting conditions and life-threatening illnesses. Design: A permeation study conducted with morphine sulphate in an ex vivo porcine buccal tissue model. Flux values and pharmacokinetic data were used to calculate the plasma values of morphine that would result following buccal administration in a 20kg child. Results: Results show that the estimated steady state plasma values of morphine sulphate following buccal administration in this model do not achieve minimum therapeutic concentration. Conclusion: These data strongly suggest that morphine sulphate is not suitable for buccal administration and that further research is needed to establish its efficacy in relief of pain in children with life-limiting conditions and life-threatening illnesses.
Oral transmucosal delivery of naratriptan Mohammed Sattar, Majella E. Lane International Journal of Pharmaceutics, 2016 Naratriptan (NAR) is currently used as the hydrochloride salt (NAR.HCl) for the treatment of migraine and is available in tablet dosage forms for oral administration. Buccal drug delivery offers a number of advantages compared with conventional oral delivery including rapid absorption, avoidance of first pass metabolism and improved patient compliance. We have previously prepared and characterised the base form of NAR and shown that it has more favourable properties for buccal delivery compared with NAR.HCl. This study describes the design and evaluation of a range of formulations for oral transmucosal delivery of NAR base. Permeation studies were conducted using excised porcine buccal tissue mounted in Franz cells. Of the neat solvents examined, Transcutol® P (TC) showed the greatest enhancement effects and was the vehicle in which NAR was most soluble. The mechanisms by which TC might promote permeation were further probed using binary systems containing TC with either buffer or Miglyol 812® (MG). Mass balance studies were also conducted for these systems. The permeation of TC as well as NAR was also monitored for TC:MG formulations. Overall, TC appears to promote enhanced membrane permeation of NAR because of its rapid uptake into the buccal tissue. Synergistic enhancement of buccal permeation was observed when TC was combined with MG and this is attributed to the increased thermodynamic activity of NAR in these formulations. Significantly enhanced permeation of NAR was achieved for TC:MG and this was also associated with less TC remaining on the tissue or in the tissue at the end of the experiment. To our knowledge this is the first report where both enhancer and active have been monitored in buccal permeation studies. The findings underline the importance of understanding the fate of vehicle components for rational formulation design of buccal delivery systems.
Preparation, characterization and buccal permeation of naratriptan Mohammed Sattar, Jonathan Hadgraft, Majella E. Lane International Journal of Pharmaceutics, 2015 Naratriptan (NAR) is currently used for the management of migraine as the hydrochloride salt (NAR.HCl) and is administered as an oral tablet. This work evaluates the feasibility of buccal delivery of NAR in order to ensure faster onset of action and avoid the side-effects associated with conventional oral formulations. We hypothesized that the unionized form of NAR would permeate buccal tissue to a greater extent than the salt. Therefore the first stage of this work required preparation of the free base from NAR.HCl. Characterisation of the base with thermal and elemental analyses confirmed its purity; logP and logD values were also determined. The pH permeation profile of NAR was also determined in the range 7.4-10. Solubility studies in non-aqueous solvents indicated that Transcutol™ (TC) and dipropylene glycol (DPG) were suitable vehicles for the free base. Maximum amounts of NAR which permeated after 6h were ∼ 130 μg/cm(2). Based on the pH permeation results and studies conducted at two different doses NAR appears to permeate porcine buccal tissue via the transcellular route. Finally, estimates of likely systemic values suggest that optimised formulations should be taken forward for in vivo evaluation.
Oral transmucosal drug delivery - Current status and future prospects Mohammed Sattar, Ossama M. Sayed, Majella E. Lane International Journal of Pharmaceutics, 2014 Oral transmucosal drug delivery (OTDD) dosage forms have been available since the 1980s. In contrast to the number of actives currently delivered locally to the oral cavity, the number delivered as buccal or sublingual formulations remains relatively low. This is surprising in view of the advantages associated with OTDD, compared with conventional oral drug delivery. This review examines a number of aspects related to OTDD including the anatomy of the oral cavity, models currently used to study OTDD, as well as commercially available formulations and emerging technologies. The limitations of current methodologies to study OTDD are considered as well as recent publications and new approaches which have advanced our understanding of this route of drug delivery.
RECENT SCHOLAR PUBLICATIONS
Effect of Disintegrants on Spironolactone Tablet Stability A Almiahi, NY Fareed, M Sattar, MA Alshawi, MN Mousa International Journal of Drug Delivery Technology 11 (3), 756-761 , 2021 2021 Citations: 3
Oral Transmucosal Drug Delivery M Sattar, ME Lane Drug Delivery Approaches: Perspectives from Pharmacokinetics and … , 2021 2021 Citations: 8
Chemical modification and characterization of chitosan for pharmaceutical applications MA Almualla, MN Mosa, M Sattar Egyptian Journal of Chemistry 64 (7), 3635-3649 , 2021 2021 Citations: 12
Stability of Dexamethasone Oral Liquid Formulations MA ALSHAWI, N ADDAI, M SATTAR, MN MOUSA, BS ALABDULLAH International Journal of Pharmaceutical Research 13 (1), 5454-5463 , 2021 2021
Spectrophotometric Determination of Nitrofurantoin in its Bulk and Pharmaceutical Formulations KS Abd-Alrassol, M Sattar, MN Mosa Systematic Reviews in Pharmacy 11 (10), 243-251 , 2020 2020 Citations: 3
Formulation and in Vitro Evaluation of Valsartan Flash Tablet M Sattar, MA Alshawi, MN Mosa Systematic Reviews in Pharmacy 11 (10), 213-219 , 2020 2020 Citations: 6
Use of buccal morphine in the management of pain in children with life-limiting conditions: Results of a laboratory study R McCulloch, M Sattar, EM Henderson, ME Lane, M Bluebond-Langner Palliative Medicine 32 (2), 554-558 , 2018 2018 Citations: 11
Oral transmucosal delivery of naratriptan M Sattar, ME Lane International Journal of Pharmaceutics 514 (1), 263–269 , 2016 2016 Citations: 7
Preparation, characterization and buccal permeation of naratriptan M Sattar, J Hadgraft, ME Lane International Journal of Pharmaceutics 493 (1-2), 146-151 , 2015 2015 Citations: 17
Oral transmucosal drug delivery–current status and future prospects M Sattar, OM Sayed, ME Lane International journal of pharmaceutics 471 (1-2), 498-506 , 2014 2014 Citations: 223
Formulation of metoprolol bilayer tablets as an oral modified release dosage form MS Jabbar, YI Khalil. Iraqi J Pharm Sci 19, 21-30 , 2010 2010 Citations: 7
MOST CITED SCHOLAR PUBLICATIONS
Oral transmucosal drug delivery–current status and future prospects M Sattar, OM Sayed, ME Lane International journal of pharmaceutics 471 (1-2), 498-506 , 2014 2014 Citations: 223
Preparation, characterization and buccal permeation of naratriptan M Sattar, J Hadgraft, ME Lane International Journal of Pharmaceutics 493 (1-2), 146-151 , 2015 2015 Citations: 17
Chemical modification and characterization of chitosan for pharmaceutical applications MA Almualla, MN Mosa, M Sattar Egyptian Journal of Chemistry 64 (7), 3635-3649 , 2021 2021 Citations: 12
Use of buccal morphine in the management of pain in children with life-limiting conditions: Results of a laboratory study R McCulloch, M Sattar, EM Henderson, ME Lane, M Bluebond-Langner Palliative Medicine 32 (2), 554-558 , 2018 2018 Citations: 11
Oral Transmucosal Drug Delivery M Sattar, ME Lane Drug Delivery Approaches: Perspectives from Pharmacokinetics and … , 2021 2021 Citations: 8
Oral transmucosal delivery of naratriptan M Sattar, ME Lane International Journal of Pharmaceutics 514 (1), 263–269 , 2016 2016 Citations: 7
Formulation of metoprolol bilayer tablets as an oral modified release dosage form MS Jabbar, YI Khalil. Iraqi J Pharm Sci 19, 21-30 , 2010 2010 Citations: 7
Formulation and in Vitro Evaluation of Valsartan Flash Tablet M Sattar, MA Alshawi, MN Mosa Systematic Reviews in Pharmacy 11 (10), 213-219 , 2020 2020 Citations: 6
Effect of Disintegrants on Spironolactone Tablet Stability A Almiahi, NY Fareed, M Sattar, MA Alshawi, MN Mousa International Journal of Drug Delivery Technology 11 (3), 756-761 , 2021 2021 Citations: 3
Spectrophotometric Determination of Nitrofurantoin in its Bulk and Pharmaceutical Formulations KS Abd-Alrassol, M Sattar, MN Mosa Systematic Reviews in Pharmacy 11 (10), 243-251 , 2020 2020 Citations: 3
Stability of Dexamethasone Oral Liquid Formulations MA ALSHAWI, N ADDAI, M SATTAR, MN MOUSA, BS ALABDULLAH International Journal of Pharmaceutical Research 13 (1), 5454-5463 , 2021 2021
