The Comparison of In Vitro Release Methods for the Evaluation of Oxytocin Release from Pluronic® F127 Parenteral Formulations

Chaibva, Faith Anesu; Walker, Roderick B.

doi:10.14227/dt140407p15

Cited by 10 publications

(6 citation statements)

References 25 publications

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“…Once again, the value for f 2 indicates that there is similarity between the two profiles, whereas the value for f 1 suggests that the profiles are different. While the use of only f 2 is considered in decision making with respect to the similarity of dissolution curves, it has been suggested that both f 1 and f 2 values should be used during formulation development studies to facilitate better decision making (24). In addition, the testing of an additional six units may also be useful to ensure that a true difference exists.…”

Section: Impact Of Mesh Screen Pore Sizementioning

confidence: 99%

Development and Assessment of a USP Apparatus 3 Dissolution Test Method for Sustained-Release Nevirapine Matrix Tablets

Mwila¹,

Khamanga²,

Walker³

2016

Dissolution Technol.

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Dissolution testing is a quality control tool used to assess batch-to-batch performance of dosage forms, thereby providing continued assurance of product quality. Analytical methods for the assessment of pharmaceutical product quality must be validated according to regulatory guidelines to ensure that tests are reliable and valid. Agitation rate, mesh pore size, surfactant concentration, and dissolution medium molarity are experimental parameters that may affect nevirapine (NVP) release and were investigated and optimized to ensure that consistent, reliable, and valid results using Apparatus 3 were produced. Agitation rate was investigated to establish an equivalent response to that observed for NVP release using Apparatus 2 at 50 rpm. A reciprocation rate of 5-10 dpm produced dissolution profiles that were similar to those observed using Apparatus 2. An increase in the molarity of the dissolution medium slightly increased the release rate of NVP, and a 50 mM buffer maintained at pH values mimicking gastrointestinal tract (GIT) conditions was selected for all experiments. With the addition of 2% sodium lauryl sulfate (SLS) to the dissolution medium, >80% NVP was released from the tablets over the test period. The NVP release rate increased with an increase in the mesh pore size; however, the extent of release was not affected by this parameter. Dissolution test samples were analyzed using HPLC, and dissolution methods were validated for NVP stability in the dissolution medium, specificity, linearity and range, repeatability, intermediate precision, and accuracy as defined by ICH. The dissolution method used for testing NVP tablets can be regarded as an appropriate tool for the evaluation of sustained-release (SR) NVP formulations and the impact of formulation composition and product quality attributes on drug release.

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Section: Impact Of Mesh Screen Pore Sizementioning

confidence: 99%

Development and Assessment of a USP Apparatus 3 Dissolution Test Method for Sustained-Release Nevirapine Matrix Tablets

Mwila¹,

Khamanga²,

Walker³

2016

Dissolution Technol.

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“…PF-127 thermosensitive gel has shown to prolong the release of various proteins and also extended stability [154,155]. In a recent work, Akash et al have evaluated sustained delivery of IL-1 receptor antagonist (IL-1Ra) from PF127 based thermosensitive gel both in vitro and in vivo [156 –158].…”

Section: Colloidal Delivery Systemsmentioning

confidence: 99%

Recent Developments in Protein and Peptide Parenteral Delivery Approaches

2014

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Discovery of insulin in the early 1900s initiated the research and development to improve the means of therapeutic protein delivery in patients. In the past decade, great emphasis has been placed on bringing protein and peptide therapeutics to market. Despite tremendous efforts, parenteral delivery still remains the major mode of administration for protein and peptide therapeutics. Other routes such as oral, nasal, pulmonary and buccal are considered more opportunistic rather than routine application. Improving biological half-life, stability and therapeutic efficacy is central to protein and peptide delivery. Several approaches have been tried in the past to improve protein and peptide in vitro/in vivo stability and performance. Approaches may be broadly categorized as chemical modification and colloidal delivery systems. In this review we have discussed various chemical approaches such as PEGylation, hyperglycosylation, mannosylation, and colloidal carriers including microparticles, nanoparticles, liposomes, carbon nanotubes and micelles for improving protein and peptide delivery. Recent developments on in situ thermosensitive gel-based protein and peptide delivery have also been described. This review summarizes recent developments on some currently existing approaches to improve stability, bioavailability and bioactivity of peptide and protein therapeutics following parenteral administration.

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“…From various previous studies, it has been proved that PF127 is safe for the sustained delivery of various proteins such as IL-2 [31], insulin [29], [32], recombinant hirudin [33], oxytocin [34] and lysozyme [35], and prolongs the stability of proteins [26]–[29]. From clinical perspective, our investigations that are derived from an experimental protocol could stimulate further clinical trials on type 2 diabetic patients to expedite therapeutic uses of PF127 for safe and effective delivery of IL-1Ra that exhibit its sustained release effects devoid of altering normal physiological functions of body and protecting the efficacy of encapsulated IL-1Ra till its delivery to the target site.…”

Section: Discussionmentioning

confidence: 99%

Sustained Delivery of IL-1Ra from PF127-Gel Reduces Hyperglycemia in Diabetic GK-Rats

et al. 2013

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Interleukin-1beta (IL-1β) is a major cause for induction of various inflammatory mechanisms that are decisively involved to provoke pathogenesis of type 2 diabetes mellitus (T2DM). Interleukin-1 receptor antagonist (IL-1Ra) a naturally occurring anti-inflammatory antagonist of IL-1β has been recently approved for treatment of T2DM but due to its short half-life, higher doses and frequent dosing intervals are required. Pluronic F-127 (PF127) has previously shown to prolong the release of various proteinous drugs and their serum half-lives. Subsequently, in our previous work, we developed a new dosage form of IL-1Ra using PF127 and investigated its in-vitro and in-vivo effects. Here in present work, we have extended this approach using diabetic Goto-kakizaki (GK) rats. We administered IL-1Ra loaded in PF127 gel subcutaneously for one month into GK rats. IL-1Ra loaded in PF127 gel exhibited a sustained and prolonged hypoglycemic effects on treated animals. Intraperitoneal glucose tolerance test (IPGTT) results showed that IL-1Ra loaded in PF127 gel increased glucose tolerance along with increased insulin sensitivity and β-cell’s secretory function in treated rats. Moreover, significant reduction in pro-insulin/insulin ratio, lipid profiles and interleukin 6 (IL-6) were also observed. Immunohistochemical analysis showed slight macrophages infiltration in pancreatic islets. Histochemical analysis revealed no PF127-induced alteration in the normal physiology of skin and kidney of treated animals. Hence, we concluded that IL-1Ra loaded in PF127 gel has potential to exhibit broad spectrum anti-inflammatory effects alleviating the symptoms of T2DM.

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The Comparison of In Vitro Release Methods for the Evaluation of Oxytocin Release from Pluronic® F127 Parenteral Formulations

Cited by 10 publications

References 25 publications

Development and Assessment of a USP Apparatus 3 Dissolution Test Method for Sustained-Release Nevirapine Matrix Tablets

Development and Assessment of a USP Apparatus 3 Dissolution Test Method for Sustained-Release Nevirapine Matrix Tablets

Recent Developments in Protein and Peptide Parenteral Delivery Approaches

Sustained Delivery of IL-1Ra from PF127-Gel Reduces Hyperglycemia in Diabetic GK-Rats

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